General Information of This Payload
Payload ID
PAY0QLDVX
Name
Monomethyl auristatin F
Synonyms
MMAF; 745017-94-1; Monomethyl Auristatin F; Monomethylauristatin F; (2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid; MonomethylauristatinF; SCHEMBL3208014; CHEMBL3359822; MonoMethyl auristatin F (MMAF); MFRNYXJJRJQHNW-DEMKXPNLSA-N; DTXSID601031563; AMY30768; EX-A1046; MFCD25976742; MONOMETHYLAURISTATIN PHENYLALANINE; AC-30596; BP-22316; HY-15579; ((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)-L-phenylalanine; (2S)-2-[(2R)-2-[(R)-[(2S)-1-[(3R,4S,5S)-4-[(2S)-N,3-dimethyl-2-[(2S)-3-methyl-2-(methylamino)butanamido]butanamido]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl](methoxy)methyl]propanamido]-3-phenylpropanoic acid; (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-Dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid; ;(2~{S})-2-[[(2~{R},3~{R})-3-methoxy-3-[(2~{S})-1-[(3~{R},4~{S},5~{S})-3-methoxy-5-methyl-4-[methyl-[(2~{S})-3-methyl-2-[[(2~{S})-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methyl-propanoyl]amino]-3-phenyl-propanoic acid; L-PHENYLALANINE, N-METHYL-L-VALYL-L-VALYL-(3R,4S,5S)-3-METHOXY-5-METHYL-4-(METHYLAMINO)HEPTANOYL-(.ALPHA.R,.BETA.R,2S)-.BETA.-METHOXY-.ALPHA.-METHYL-2-PYRROLIDINEPROPANOYL-
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Target Microtubule (MT)
Structure
Formula
C39H65N5O8
Isosmiles
CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)O)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC
PubChem CID
10395173
InChI
InChI=1S/C39H65N5O8/c1-12-25(6)34(43(9)38(48)33(24(4)5)42-37(47)32(40-8)23(2)3)30(51-10)22-31(45)44-20-16-19-29(44)35(52-11)26(7)36(46)41-28(39(49)50)21-27-17-14-13-15-18-27/h13-15,17-18,23-26,28-30,32-35,40H,12,16,19-22H2,1-11H3,(H,41,46)(H,42,47)(H,49,50)/t25-,26+,28-,29-,30+,32-,33-,34-,35+/m0/s1
InChIKey
MFRNYXJJRJQHNW-DEMKXPNLSA-N
IUPAC Name
(2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid
Pharmaceutical Properties
Molecule Weight
732
Polar area
167
Complexity
1160
xlogp Value
2.1
Heavy Count
52
Rot Bonds
21
Hbond acc
9
Hbond Donor
4
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 10 nM
HT-29 cells
Colon adenocarcinoma
CVCL_0320 
[1]
Half Maximal Inhibitory Concentration (IC50) 105 nM
H3396 cells
Breast carcinoma
CVCL_D348 
[1]
Half Maximal Inhibitory Concentration (IC50) 137 nM
HL-60 cells
Adult acute myeloid leukemia
CVCL_0002 
[1]
Half Maximal Inhibitory Concentration (IC50) 2880 nM
HCT 116 cells
Colon carcinoma
CVCL_0291 
[1]
Half Maximal Inhibitory Concentration (IC50) 5.3 nM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[2]
Half Maximal Inhibitory Concentration (IC50) 7 nM
Hep-G2 cells
Hepatoblastoma
CVCL_0027 
[3]
Half Maximal Inhibitory Concentration (IC50) 8.8 nM
BT474-M1 cells
Invasive breast carcinoma
CVCL_0179 
[2]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
GPC-1-ADC [Investigative]
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 22.63% Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (1 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model Pancreatic cancer PDX model
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 29.66% Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (3 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model Pancreatic cancer PDX model
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.22% Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (10 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model Pancreatic cancer PDX model
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.97% Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour-bearing mice were intravenously administered PBS, control ADC or GPC-1-ADC (1 mg/kg) on days 0, 4, 8 and 12.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85% Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour-bearing mice were intravenously administered PBS, control ADC or GPC-1-ADC (3 mg/kg) on days 0, 4, 8 and 12.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96% Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour-bearing mice were intravenously administered PBS, control ADC (10 mg/kg ) or GPC-1-ADC (10 mg/kg) on days 0, 4, 8 and 12, once every 4 days for a total of four doses.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
Positive GPC-1 expression (GPC-1 +++/++)
Method Description
IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.24 nM
Positive GPC-1 expression (GPC-1 +++/++)
Method Description
IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model Pancreatic ductal adenocarcinoma T3M-4 cells CVCL_4056
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative GPC-1 expression (GPC-1 -)
Method Description
IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model Pancreatic ductal adenocarcinoma SUIT-2 cells CVCL_3172
ASG-15MF [Investigative]
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 62.90% High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description
PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,ASG-15MF was dosed at 0.25 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model Bladder cancer PDX model (PDX: AG-B8)
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 63.40% High SLITRK6 expression (SLITRK6+++; IHC H-score=230)
Method Description
PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,ASG-15MF was dosed at 0.5 mg/kg,2x per week i.v in AG-B7 PDX model. The last dose was given on day 21.
In Vivo Model Bladder cancer PDX model (PDX: AG-B7)
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80% High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description
PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,ASG-15MF was dosed at 0.5 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model Bladder cancer PDX model (PDX: AG-B8)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.20% Moderate SLITRK6 expression (SLITRK6++; IHC H-score=185)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. ASG-15MF was administered twice weekly at 3 mg/kg (n = 6) starting when the tumor volume reached approximately 200 mm3.
In Vivo Model NCI-322M CDX model
In Vitro Model Lung cancer NCI-322M cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.30% High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of ASG-15MF, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model Bladder cancer CDX model
In Vitro Model Bladder cancer Bladder cancer cells Homo sapiens
HuM25-mcMMAF-E2 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Tumor Growth Inhibition value (TGI)
0%
Positive LRRC15 expression (LRRC15 +++/++)
Method Description
LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-MCMMAF-E2 (12 mg/kg) was demonstrated in PANC-1 xenografts.
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Tumor Growth Inhibition value (TGI)
8.47%
High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description
LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-MCMMAF-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model EBC-1 CDX model
In Vitro Model Lung squamous cell carcinoma EBC-1 cells CVCL_2891
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 - 0.10 nM
Positive LRRC15 expression (LRRC15 +++/++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model Colon carcinoma HCT 116 cells CVCL_0291
GPC-1 ADC 1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 21.71% Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (1 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 28.13% Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (1 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 3 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 33.65% Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (3 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 4 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 43.94% Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (3 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 5 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.65% Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (10 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 6 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.49% Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (10 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive GPC1 expression (GPC1 +++/++)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive GPC1 expression (GPC1 +++/++)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 3 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative GPC1 expression (GPC1 -)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Ovarian clear cell adenocarcinoma RMG-I cells CVCL_1662
Anti-BCMA J6M0-mcMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 24.38% High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model NCI-H929 CDX model
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [8]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 65.09% Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1S CDX model
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [8]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 66.25% Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
Experiment 4 Reporting the Activity Date of This ADC [8]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.86% High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 3 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1R CDX model
In Vitro Model Plasma cell myeloma MM1.R cells CVCL_8794
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
29.28 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
55.55 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
159.7 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.46 uM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Ab3-mcMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.23% Positive EGFR expression (EGFR+++/++)
Method Description
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model EBC-1 CDX model
In Vitro Model Lung squamous cell carcinoma EBC-1 cells CVCL_2891
HA15-1C25F [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.90% High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-1c25F, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model Bladder cancer CDX model
In Vitro Model Bladder cancer Bladder cancer cells Homo sapiens
HA15-1ABE16F [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 44.70% High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-1abe16F, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model Bladder cancer CDX model
In Vitro Model Bladder cancer Bladder cancer cells Homo sapiens
WO2017089890A1 ADC34 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.68% Moderate HER2 expression (HER2++)
Method Description
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.39% Moderate HER2 expression (HER2++)
Method Description
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Ch14.18-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [11]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.74% Positive GD2 expression (GD2+++/++)
Method Description
When tumors reached 50 mm3 volume. Three groups received intravenous injections of 100 ug (5 mg/kg) ch14.18-MMAE, ch14.18-MMAF, or naked antibody for five times with an interval of 4 days, and the control group was injected with PBS.
In Vivo Model EL-4 CDX model
In Vitro Model Thymoma EL4 cells CVCL_0255
Experiment 2 Reporting the Activity Date of This ADC [11]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 74.95% Positive GD2 expression (GD2+++/++)
Method Description
When tumors reached 50 mm3 volume. Three groups received intravenous injections of 100 ug (5 mg/kg) ch14.18-MMAE, ch14.18-MMAF, or naked antibody for five times with an interval of 4 days, and the control group was injected with PBS.
In Vivo Model B78-D14 CDX model
In Vitro Model Amelanotic melanoma B78-D14 cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 38 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Amelanotic melanoma B78-D14 cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Thymoma EL4 cells CVCL_0255
Experiment 3 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.81 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Neuroblastoma IMR-32 cells CVCL_0346
Experiment 4 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.27 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Amelanotic melanoma COLO 38 cells CVCL_3934
Experiment 5 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.84 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Glioblastoma T98G cells CVCL_0556
Experiment 6 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.3 nM
Moderate GD2 expression (GD2++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma U2OS cells CVCL_0042
Experiment 7 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.7 nM
Moderate GD2 expression (GD2++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Pleural malignant mesothelioma MS-1 [Human mesothelioma] cells CVCL_E993
Experiment 8 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.8 nM
Moderate GD2 expression (GD2++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Invasive breast carcinoma Hs 578T cells CVCL_0332
Experiment 9 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Astrocytoma 1321N1 cells CVCL_0110
Experiment 10 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 11 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 20 nM Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma MG-63 cells CVCL_0426
Experiment 12 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Malignant neoplasms of the mouse mammary gland M3 cells CVCL_4Y25
Experiment 13 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Melanoma B16 cells CVCL_F936
Experiment 14 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 15 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 16 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma HOS cells CVCL_0312
Experiment 17 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Glioblastoma U-87MG cells CVCL_0022
Experiment 18 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Neuroblastoma NGP-127 cells CVCL_UF75
Experiment 19 Reporting the Activity Date of This ADC [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 40 nM Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Bone marrow neuroblastoma SH-SY5Y cells CVCL_0019
Experiment 20 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.02 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Thymoma EL4 cells CVCL_0255
Experiment 21 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.02 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Amelanotic melanoma B78-D14 cells Homo sapiens
Experiment 22 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.19 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Glioblastoma T98G cells CVCL_0556
Experiment 23 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.25 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Neuroblastoma IMR-32 cells CVCL_0346
Experiment 24 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.3 nM
Moderate GD2 expression (GD2++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Pleural malignant mesothelioma MS-1 [Human mesothelioma] cells CVCL_E993
Experiment 25 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.3 nM
High GD2 expression (GD2+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Amelanotic melanoma COLO 38 cells CVCL_3934
Experiment 26 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.3 nM
Moderate GD2 expression (GD2++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma U2OS cells CVCL_0042
Experiment 27 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.48 nM
Moderate GD2 expression (GD2++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Invasive breast carcinoma Hs 578T cells CVCL_0332
Experiment 28 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
1 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Astrocytoma 1321N1 cells CVCL_0110
Experiment 29 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
5.3 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 30 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
5.3 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 31 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
5.3 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Bone marrow neuroblastoma SH-SY5Y cells CVCL_0019
Experiment 32 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
7.3 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma MG-63 cells CVCL_0426
Experiment 33 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
12.4 nM
Low GD2 expression (GD2+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Glioblastoma U-87MG cells CVCL_0022
Experiment 34 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20) > 20 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Malignant neoplasms of the mouse mammary gland M3 cells CVCL_4Y25
Experiment 35 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20) > 20 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Melanoma B16 cells CVCL_F936
Experiment 36 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20) > 20 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 37 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20) > 20 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma HOS cells CVCL_0312
Experiment 38 Reporting the Activity Date of This ADC [11]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20) > 20 nM Negative GD2 expression (GD2-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Neuroblastoma NGP-127 cells CVCL_UF75
RBGO1-mcF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 60% Positive RAGE expression (RAGE+++/++)
Method Description
Nude athymic mice were divided into three treatment groups of six mice each. Mice were treated with PBS (control) or RBGO1 ADC at either 3 mg/kg or 20mg/kg N intravenous injection. Bodyweight was measured at days 3, 6, 8, 13, 17 and 21 and mouse health assessed daily.
In Vivo Model HEC-1-A CDX model
In Vitro Model Endometrial adenocarcinoma HEC-1-A cells CVCL_0293
M25ADCMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [13]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 62.30% Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 150 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for a total of 4 doses at 5 mg/kg.
In Vivo Model M28 CDX model
In Vitro Model Pleural malignant mesothelioma M28K cells CVCL_8106
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.16% Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 250 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for a total of 4 doses at 5 mg/kg.
In Vivo Model M28 CDX model
In Vitro Model Pleural malignant mesothelioma M28K cells CVCL_8106
Experiment 3 Reporting the Activity Date of This ADC [13]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.72% Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 500 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for a total of 4 doses at 5 mg/kg.
In Vivo Model M28 CDX model
In Vitro Model Pleural malignant mesothelioma M28K cells CVCL_8106
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.4 nM
Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model Pleural malignant mesothelioma M28K cells CVCL_8106
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Effective Concentration (EC50)
36 nM
Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model Pleural sarcomatoid mesothelioma VAMT-1 cells CVCL_A731
Experiment 3 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model Normal HS-27 cells CVCL_0E34
Experiment 4 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model Normal HS775Li cells Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model Normal HK-2 [Human kidney] cells CVCL_0302
HA15-10AC14F [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 64.30% High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description
CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-10ac14F, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model Bladder cancer CDX model
In Vitro Model Bladder cancer Bladder cancer cells Homo sapiens
GPC1-ADC-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [14]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.70% High GPC1 expression (GPC1+++)
Method Description
The SCID mice were subcutaneously inoculated with BxPC-3-GPC1-KO-Luc#15 cells and then intravenously treated with PBS, 10-mg/kg control-ADC, or 10-mg/kg humanized GPC1-ADC(MMAE) twice a week for a total of four times.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
hBU12-mcMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 76.44% Positive CD19 expression (CD19+++/++)
Method Description
To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model DOHH1 CDX model
In Vitro Model Diffuse large B-cell lymphoma germinal center B-cell type DoHH2 cells CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.21% Positive CD70 expression (CD70+++/++)
Method Description
To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model 786-O CDX model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
34 ng/mL
Positive CD70 expression (CD70+++/++)
Method Description
Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
LCB14-0648 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.97% Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 2 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.16% Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 5 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.70% Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 10 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110 ng/mL
Positive CD19 expression (CD19 +++/++)
Method Description
Raji cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 ug/mL Negative CD19 expression (CD19 -)
Method Description
K562 cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°Cin 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
Ab1-mcMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.39% Positive EGFR expression (EGFR+++/++)
Method Description
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model EBC-1 CDX model
In Vitro Model Lung squamous cell carcinoma EBC-1 cells CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.40% Positive EGFR expression (EGFR+++/++)
Method Description
Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
In Vivo Model NCI-H1703 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H1703 cells CVCL_1490
IC1-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [17]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.30% Positive ICAM1 expression (ICAM1 +++/++)
Method Description
IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model MDA-MB-231 CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC [17]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99% Positive ICAM1 expression (ICAM1 +++/++)
Method Description
IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model MDA-MB-436 CDX model
In Vitro Model Metastasis of ductal carcinoma MDA-MB-436 cells CVCL_0623
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.3 pM
Positive ICAM1 expression (ICAM1 +++/++)
Method Description
In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model Metastasis of ductal carcinoma MDA-MB-436 cells CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
68.7 pM
Positive ICAM1 expression (ICAM1 +++/++)
Method Description
In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
Positive ICAM1 expression (ICAM1 +++/++)
Method Description
In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model Breast carcinoma MDA-MB-157 cells CVCL_0618
1F6-Val-Cit-PABC-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Tumor Growth Inhibition value (TGI)
84.59%
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model DBTRG-05MG glioblastoma cell line xenograft model
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Tumor Growth Inhibition value (TGI)
85.01%
Positive TNF expression (TNF+++/++)
Method Description
1 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Tumor Growth Inhibition value (TGI)
93.25%
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.90±2.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.10±2.70 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.10±3.60 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
WO2007011968A2 c1F6-9b [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.08% Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
An in vivo therapy experiments with c1F6-9b was undertaken in nude mice with subcutaneous 786-O cells. The animals (5 per group)were treated with a single intravenous dose of c1F6-9b at 0.75 mg/kg (mAb component) on day 14.
In Vivo Model 786-O CDX model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.93% Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
An in vivo therapy experiments with c1F6-9b was undertaken in nude mice with subcutaneous 786-O cells. The animals (5 per group)were treated with a single intravenous dose of c1F6-9b at 1.5 mg/kg (mAb component) on day 14.
In Vivo Model 786-O CDX model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [19]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94% Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
An in vivo therapy experiments with c1F6-9b was undertaken in nude mice with subcutaneous 786-O cells. The animals (5 per group)were treated with a single intravenous dose of c1F6-9b at 3 mg/kg (mAb component) on day 14.
In Vivo Model 786-O CDX model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.2 nM
Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50 nM Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Anti-BCMA 15B2WT-mcMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.16% Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
WO2017089890A1 ADC23 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.52% Moderate HER2 expression (HER2++)
Method Description
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.72% Moderate HER2 expression (HER2++)
Method Description
JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.35 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.44 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
HER2-acetal-ADC 12 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive HER2 expression (HER2 +++/++)
Method Description
NOD-SCID mice with heterotopic SKBR-3 tumor xenografts were injected intravenously with either ADC 12 (1.12 mg/kg; group A), PBS 1x (vehicle; group B) or Kadcyla (1.12 mg/kg; group C) and tumor volume was measured every 2-3 days for 30 days.
In Vivo Model SKBR-3 CDX model
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.22 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2-)
Method Description
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
EVCit ADC 3c [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive HER2 expression (HER2+++/++)
Method Description
EVCit ADC 3c (3 mg/kg, single dose) induces efficient tumor cell killing in cell line-derived models of KPL-4 cells with HER2 expression with high expression.
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 2 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2-)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
VCit ADC 3a [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive HER2 expression (HER2+++/++)
Method Description
VCit ADC 3a (3 mg/kg, single dose) induces efficient tumor cell killing in cell line-derived models of KPL-4 cells with HER2 expression with high expression.
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 2 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2-)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
HBU12-mc-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% Positive CD19 expression (CD19 +++/++)
Method Description
We tested the activity of anti-human CD19-targeted ADCs in a human CD19+ Ramos non-Hodgkin lymphoma xenograft tumor model.
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
WO2017089895A1 ADC34 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
58.23%
Positive HER2 expression (HER2+++/++)
Method Description
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
87.94%
Positive HER2 expression (HER2+++/++)
Method Description
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC23 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
96.08%
Positive HER2 expression (HER2+++/++)
Method Description
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
99.23%
Positive HER2 expression (HER2+++/++)
Method Description
JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.21 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.35 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.44 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Trastuzumab DVD-ADC [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [24]
Efficacy Data Inhibition rate (100nM)
0%
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC [24]
Efficacy Data Inhibition rate (100nM)
0%
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [24]
Efficacy Data Inhibition rate (100nM) > 50% High HER2 expression (HER2+++); Moderate TRKB expression (TRKB++)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
ZHER2-ABD-mcMMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 nM
High HER2 expression (HER2 +++)
Method Description
HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.2 nM
High HER2 expression (HER2 +++)
Method Description
HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model Breast adenocarcinoma AU565 cells CVCL_1074
Experiment 3 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.2 nM
High HER2 expression (HER2 +++)
Method Description
HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12 nM
High HER2 expression (HER2 +++)
Method Description
HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
215 nM
Moderate HER2 expression (HER2 ++)
Method Description
HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
WO2017089890A1 ADC77 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC62 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC77 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC50 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC44 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC42 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC38 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC6 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.38 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC53 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC50 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC44 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC42 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC38 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC6 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.07 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.38 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC55 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.07 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2007011968A2 cAC10-9b [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50 nM Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50 nM Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
WO2017089895A1 ADC69 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive CD19 expression (CD19+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive CD19 expression (CD19+++/++)
Method Description
Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.14 nM
Positive CD19 expression (CD19+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD19 expression (CD19-)
Method Description
K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
WO2017089895A1 ADC16 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.07 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.26 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Anti-HER2 DVD-IgG1_MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Anti-HER2 DVD-IgG1-h38c2-K99C_MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
WO2017089890A1 ADC16 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.26 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.31 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC62 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.29 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.29 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC69 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive CD19 expression (CD19+++/++)
Method Description
Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD19 expression (CD19-)
Method Description
Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
WO2017089890A1 ADC14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.31 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.14 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.15 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.42 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Esophageal adenocarcinoma OE19 cells CVCL_1622
Experiment 6 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.75 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.19 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.37 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC18 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.32 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.97 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.21 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC18 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.32 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.97 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.21 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.1 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.18 nM
Positive HER2 expression (HER2+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.33 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative EGFR expression (EGFR-)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Low EGFR expression (EGFR+)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.14 nM
High HER2 expression (HER2 +++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.42 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

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In Vitro Model Esophageal adenocarcinoma OE19 cells CVCL_1622
Experiment 4 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.75 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.19 nM
High HER2 expression (HER2+++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ADC14-0810 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [27]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.25 nM
Moderate EGFR expression (EGFR ++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [27]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.54 nM
High EGFR expression (CD19 +++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [27]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Low EGFR expression (EGFR +)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC76 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.27 nM
Moderate HER2 expression (HER2++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC76 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.27 nM
Positive HER2 expression (HER2+++/++)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative HER2 expression (HER2-)
Method Description
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Anti-HER2 DVD-Fab_MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.33 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Anti-HER2 DVD-Fab-h38c2-K99C_MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.33 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
WO2017089890A1 ADC64 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.47 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.3 nM
High EGFR expression (EGFR+++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative EGFR expression (EGFR-)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC64 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.47 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.3 nM
High EGFR expression (EGFR+++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Low EGFR expression (EGFR+)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
FOLR1-Mal-Caproyl-Val-Cit-PABC-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1 nM
High FOLR1 expression(FOLR1+++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative FOLR1 expression(FOLR1-)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Osteosarcoma SJSA-1 cells CVCL_1697
Experiment 3 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Low FOLR1 expression(FOLR1+)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Moderate FOLR1 expression(FOLR1++)
Method Description
Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model Lung non-small cell carcinoma NCI-H2110 cells CVCL_1530
WO2017089890A1 ADC72 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.78 nM
Positive CD20 expression (CD20+++/++)
Method Description
Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD20 expression (CD20-)
Method Description
Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
WO2017089895A1 ADC72 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.78 nM
Positive CD20 expression (CD20+++/++)
Method Description
Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2 nM
Positive CD20 expression (CD20+++/++)
Method Description
ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.85 nM
Positive CD20 expression (CD20+++/++)
Method Description
ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD20 expression (CD20-)
Method Description
K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
WO2021044208A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.07 nM
Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 2 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 4 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Experiment 5 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
WO2017089890A1 ADC70 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.56 nM
Positive CD20 expression (CD20+++/++)
Method Description
Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD20 expression (CD20-)
Method Description
Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
WO2017089895A1 ADC70 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.56 nM
Positive CD20 expression (CD20+++/++)
Method Description
Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD20 expression (CD20-)
Method Description
K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
WO2021044208A1 ADC9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 3 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 nM Positive ROR1 expression (ROR1+++/++)
Method Description
In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
HER2-acetal-ADC 11 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
22 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [20]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
100 nM
Negative HER2 expression (HER2-)
Method Description
Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
WO2017089890A1 ADC67 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD19 expression (CD19-)
Method Description
Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Positive CD19 expression (CD19+++/++)
Method Description
Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
WO2017089895A1 ADC67 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Negative CD19 expression (CD19-)
Method Description
K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.3 nM Positive CD19 expression (CD19+++/++)
Method Description
Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
1F6-Asn- (D)Lys-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
1F6-Met- (D)Lys-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
123 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Anti-CD19(LC)-G7VIM-2i [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110 ng/mL
Positive CD19 expression (CD19 +++/++)
Method Description
Raji cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10 ug/mL Negative CD19 expression (CD19 -)
Method Description
K562 cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°Cin 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
DAR4-ARC-ADC [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [30]
Efficacy Data Half Maximal Effective Concentration (EC50)
25 pM
Positive CLL-1 expression (CLL-1+++/++)
Method Description
In vitro cytotoxicity of the anti-hCLL-1 ARC-ADCs was then evaluated using human AML cell lines U937 (CLL-1+) and KG1a (CLL-1-1).
In Vitro Model Adult acute monocytic leukemia U-937 cells CVCL_0007
DAR2-ARC-ADC [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [30]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.9 nM
Positive CLL-1 expression (CLL-1+++/++)
Method Description
In vitro cytotoxicity of the anti-hCLL-1 ARC-ADCs was then evaluated using human AML cell lines U937 (CLL-1+) and KG1a (CLL-1-1).
In Vitro Model Adult acute monocytic leukemia U-937 cells CVCL_0007
Anti-CD276 mAb-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [31]
Efficacy Data Tumor Growth lnhibition value (TGl)
64.10%
Method Description
To evaluate the synergetic anti-NSCLC efficacy of CD276 mAb-MMAF, about 3 × 106 mouse LLC-FLuc cells were s.c. injected into C57BL mice to establish immunocompetent models. The mice were i.v. injected with saline (vehicle, control), 12 mg/kg anti-CD276 mAb (control), and 12 and 24 mg/kg anti-CD276 mAb-MMAF (n = 6). (12 mg/kg)
In Vivo Model H460-FLuc cells into nude mice model
Experiment 2 Reporting the Activity Date of This ADC [31]
Efficacy Data Tumor Growth lnhibition value (TGl)
91.90%
Method Description
To evaluate the synergetic anti-NSCLC efficacy of CD276 mAb-MMAF, about 3 × 106 mouse LLC-FLuc cells were s.c. injected into C57BL mice to establish immunocompetent models. The mice were i.v. injected with saline (vehicle, control), 12 mg/kg anti-CD276 mAb (control), and 12 and 24 mg/kg anti-CD276 mAb-MMAF (n = 6). (24 mg/kg)
In Vivo Model H460-FLuc cells into nude mice model
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [31]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
32.5 nM
High CD276 expression (CD276 +++)
Method Description
The cytotoxicity assay was performed using human NSCLC cell line H460-FLuc and mouse LLC-FLuc. With different cell division rates, 3000 H460-FLuc cells or 1000 LLC-FLuc cells with 200 uL of RPMI-1640 or a DMEM complete growth medium were seeded into each well in the 96-well plates. The cells were incubated at 37 °C in a CO2 incubator for 24 h, followed by the addition of free MMAF or ADC at dosages of 0, 10, 20, 40, 80, 120, 160, and 200 nM. The 3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide Cell Proliferation Assay (MTT Assay) was performed following the biomanufacturer procedure after 5-day treatment. At the end of treatment, the spent medium was removed and replaced with 100 uL of the fresh culture medium supplemented with 10 uL of the MTT reagent in each well. After 2 h of incubation in the dark, 100 uL of the detergent reagent was added to each well until a purple color was developed. The OD value was read at 590 nm using a SpectraMax iD3 plate reader (San Jose, CA, USA), and IC50 values were calculated.

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In Vitro Model Lung large cell carcinoma H460 cells (Human) CVCL_0459
Experiment 2 Reporting the Activity Date of This ADC [31]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
60.5 nM
Low CD276 expression (CD276+)
Method Description
The cytotoxicity assay was performed using human NSCLC cell line H460-FLuc and mouse LLC-FLuc. With different cell division rates, 3000 H460-FLuc cells or 1000 LLC-FLuc cells with 200 uL of RPMI-1640 or a DMEM complete growth medium were seeded into each well in the 96-well plates. The cells were incubated at 37 °C in a CO2 incubator for 24 h, followed by the addition of free MMAF or ADC at dosages of 0, 10, 20, 40, 80, 120, 160, and 200 nM. The 3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide Cell Proliferation Assay (MTT Assay) was performed following the biomanufacturer procedure after 5-day treatment. At the end of treatment, the spent medium was removed and replaced with 100 uL of the fresh culture medium supplemented with 10 uL of the MTT reagent in each well. After 2 h of incubation in the dark, 100 uL of the detergent reagent was added to each well until a purple color was developed. The OD value was read at 590 nm using a SpectraMax iD3 plate reader (San Jose, CA, USA), and IC50 values were calculated.

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In Vitro Model Malignant tumors of the mouse pulmonary system LCC cells (Mouse) CVCL_5653
37146146 IC1-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [32]
Efficacy Data Tumor Growth lnhibition value (TGl)
84.30%
Method Description
For the in vivo efficacy studies, orthotopic TNBC tumors (MDA-MB-436 or MDA-MB-231) were established in 6- to 8-week-old female nude mice as described above. Tumors were grown to reach 100 mm3 for standard setting treatment or 500 mm3 for late-stage treatment. Then, tumor-bearing mice were randomly divided into various treatment groups (n ≥ 5 per group) and received treatment of PBS (sham), free Dox, IC1 Ab, IC1-MMAE, or IC1-MMAF at an equivalent dosage of 5 mg/kg per week for 3 weeks via tail vein injection. Tumor growth was monitored weekly using a caliper. At the end point, animals were euthanized with CO2 and orthotopic tumors were excised to measure their mass. In dosage-dependent experiments, three ascending IC1-MMAE dosages (1, 5, and 10 mg/kg) were evaluated in orthotopic TNBC tumors (MDA-MB-436) using the same protocol. Then, mice were euthanized with CO2 and 500 ul of mouse blood was collected immediately via cardiac puncture. Collected blood was incubated for 20 min at RT to allow clotting, and then mouse serum was isolated after centrifuging at 2000g for 10 min in a refrigerated centrifuge. Serum levels of ALT, AST, creatinine, and BUN were determined using their activity assay kits purchased from Sigma-Aldrich (St. Louis, MO, USA) with provided protocols. In MTD studies, the in vivo tolerability of IC1-MMAE was examined in 6- to 8-week-old female BALB/c mice. Healthy mice were randomized into various treatment groups (n = 10 per group) and received intravenous injections of IC1-MMAE at three ascending dosages (25, 50, and 75 mg/kg) for one injection. After injection, mouse body weight loss was used as the acute toxicity indicator and was closely monitored for up to 14 days.

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In Vivo Model Refractory MDA-MB-231 tumor model
Experiment 2 Reporting the Activity Date of This ADC [32]
Efficacy Data Tumor Growth lnhibition value (TGl)
99%
Method Description
For the in vivo efficacy studies, orthotopic TNBC tumors (MDA-MB-436 or MDA-MB-231) were established in 6- to 8-week-old female nude mice as described above. Tumors were grown to reach 100 mm3 for standard setting treatment or 500 mm3 for late-stage treatment. Then, tumor-bearing mice were randomly divided into various treatment groups (n ≥ 5 per group) and received treatment of PBS (sham), free Dox, IC1 Ab, IC1-MMAE, or IC1-MMAF at an equivalent dosage of 5 mg/kg per week for 3 weeks via tail vein injection. Tumor growth was monitored weekly using a caliper. At the end point, animals were euthanized with CO2 and orthotopic tumors were excised to measure their mass. In dosage-dependent experiments, three ascending IC1-MMAE dosages (1, 5, and 10 mg/kg) were evaluated in orthotopic TNBC tumors (MDA-MB-436) using the same protocol. Then, mice were euthanized with CO2 and 500 ul of mouse blood was collected immediately via cardiac puncture. Collected blood was incubated for 20 min at RT to allow clotting, and then mouse serum was isolated after centrifuging at 2000g for 10 min in a refrigerated centrifuge. Serum levels of ALT, AST, creatinine, and BUN were determined using their activity assay kits purchased from Sigma-Aldrich (St. Louis, MO, USA) with provided protocols. In MTD studies, the in vivo tolerability of IC1-MMAE was examined in 6- to 8-week-old female BALB/c mice. Healthy mice were randomized into various treatment groups (n = 10 per group) and received intravenous injections of IC1-MMAE at three ascending dosages (25, 50, and 75 mg/kg) for one injection. After injection, mouse body weight loss was used as the acute toxicity indicator and was closely monitored for up to 14 days.

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In Vivo Model MDA-MB-436 orthotopic TNBC model
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [32]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
7.3 pM
Moderate ICAM1 expression (ICAM1++)
Method Description
Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and allowed to attach overnight. Then, cells were treated with four different ICAM1 ADCs (IC1-DM1, IC1-DM4, IC1-MMAE, and IC1-MMAF) at different drug concentrations ranging from 0 to 10 ug/ml using a serial dilution factor of 10. After cells were cultured for another 48 hours, the cytotoxicity was determined by CCK-8 assay. The plate was read at the absorbance wavelength of 450 nm using a Molecular Devices SpectraMax microplate reader (San Jose, CA, USA). Cell viability was determined by comparing the absorbance of cells incubated with drugs to that of the control cells incubated without the presence of the drug.

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In Vitro Model Metastasis of ductal carcinoma MDA-MB-436 cells CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC [32]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
68.7 pM
High ICAM1 expression (ICAM1 +++)
Method Description
Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and allowed to attach overnight. Then, cells were treated with four different ICAM1 ADCs (IC1-DM1, IC1-DM4, IC1-MMAE, and IC1-MMAF) at different drug concentrations ranging from 0 to 10 ug/ml using a serial dilution factor of 10. After cells were cultured for another 48 hours, the cytotoxicity was determined by CCK-8 assay. The plate was read at the absorbance wavelength of 450 nm using a Molecular Devices SpectraMax microplate reader (San Jose, CA, USA). Cell viability was determined by comparing the absorbance of cells incubated with drugs to that of the control cells incubated without the presence of the drug.

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In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [32]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
116 pM
Moderate ICAM1 expression (ICAM1++)
Method Description
Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and allowed to attach overnight. Then, cells were treated with four different ICAM1 ADCs (IC1-DM1, IC1-DM4, IC1-MMAE, and IC1-MMAF) at different drug concentrations ranging from 0 to 10 ug/ml using a serial dilution factor of 10. After cells were cultured for another 48 hours, the cytotoxicity was determined by CCK-8 assay. The plate was read at the absorbance wavelength of 450 nm using a Molecular Devices SpectraMax microplate reader (San Jose, CA, USA). Cell viability was determined by comparing the absorbance of cells incubated with drugs to that of the control cells incubated without the presence of the drug.

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In Vitro Model Breast carcinoma MDA-MB-157 cells CVCL_0618
C1.18 DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
146C: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
58.62 nM
High C10orf54 expression (C10orf54 +++)
Method Description
146C: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
146C: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 146C: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
164A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.3 nM
High C10orf54 expression (C10orf54 +++)
Method Description
164A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
62.86 nM
High C10orf54 expression (C10orf54 +++)
Method Description
164A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 164A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
208A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.31 nM
High C10orf54 expression (C10orf54 +++)
Method Description
208A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
208A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 208A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
215A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.43 nM
High C10orf54 expression (C10orf54 +++)
Method Description
215A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
215A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 215A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
230A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3.06 nM
High C10orf54 expression (C10orf54 +++)
Method Description
230A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
230A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 230A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
259A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.56 nM
High C10orf54 expression (C10orf54 +++)
Method Description
259A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
259A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 259A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
305A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.81 nM
High C10orf54 expression (C10orf54 +++)
Method Description
305A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
305A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 305A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
353A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.51 nM
High C10orf54 expression (C10orf54 +++)
Method Description
353A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
353A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 53A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
5B: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.01 nM
High C10orf54 expression (C10orf54 +++)
Method Description
5B: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM High C10orf54 expression (C10orf54 +++)
Method Description
5B: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 5B: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.001 nM High C10orf54 expression (C10orf54 +++)
Method Description
175A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.16 nM
High C10orf54 expression (C10orf54 +++)
Method Description
175A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
7.83 nM
High C10orf54 expression (C10orf54 +++)
Method Description
175A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
CN114230664B 175A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.02 nM
High C10orf54 expression (C10orf54 +++)
Method Description
76E1: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.08 nM
High C10orf54 expression (C10orf54 +++)
Method Description
76E1: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.11 nM
High C10orf54 expression (C10orf54 +++)
Method Description
76E1: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
EP4461318A2 anti-PSMA ADC13 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.047 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

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In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
EP4461318A2 anti-PSMA ADC14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.049 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

   Click to Show/Hide
In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
40410803 16B10-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.05&#1770.03 nM
Method Description
All cell lines were cultured at 37oC in a humidified atmosphere in the presence of 5% CO2 and 95% air in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% FBS containing high glucose (4500 mg/liter) and antibiotics (penicillin 100 U/ml, streptomycin 100 ug/ml). Cells were tested for authenticity by STR at the Hematology Service of the University of Salamanca. NP29 and NP31 cells were obtained from patient samples by Dr. Gabriel Capellá. Cell proliferation experiments were conducted using a Z1 Coulter Particle Counter as described previously [28, 29]. Apoptosis and cell cycle analyses were performed as described [30]. The KRAS mutation status of genomic DNA isolated using TRIzol (Thermo Fisher Scientific) from Capan-1, IMIM-PC1, IMIM-PC2, SKPC1, NP29, and NP31 cell lines was analyzed with the KRAS Mutation Test v2 (LSR) on the Cobas® platform (Roche Diagnostics) by PCR using the Cobas® z 480 analyzer (Roche). The resulting data are presented in Supplementary Table 1.

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In Vitro Model Pancreatic ductal adenocarcinoma SKPC1 cells CVCL_4054
Experiment 2 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.15&#1770.04 nM
Method Description
All cell lines were cultured at 37oC in a humidified atmosphere in the presence of 5% CO2 and 95% air in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% FBS containing high glucose (4500 mg/liter) and antibiotics (penicillin 100 U/ml, streptomycin 100 ug/ml). Cells were tested for authenticity by STR at the Hematology Service of the University of Salamanca. NP29 and NP31 cells were obtained from patient samples by Dr. Gabriel Capellá. Cell proliferation experiments were conducted using a Z1 Coulter Particle Counter as described previously [28, 29]. Apoptosis and cell cycle analyses were performed as described [30]. The KRAS mutation status of genomic DNA isolated using TRIzol (Thermo Fisher Scientific) from Capan-1, IMIM-PC1, IMIM-PC2, SKPC1, NP29, and NP31 cell lines was analyzed with the KRAS Mutation Test v2 (LSR) on the Cobas® platform (Roche Diagnostics) by PCR using the Cobas® z 480 analyzer (Roche). The resulting data are presented in Supplementary Table 1.

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In Vitro Model Pancreatic carcinoma NP29 cells CVCL_E3BR
Experiment 3 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.32&#1770.08 nM
Method Description
All cell lines were cultured at 37oC in a humidified atmosphere in the presence of 5% CO2 and 95% air in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% FBS containing high glucose (4500 mg/liter) and antibiotics (penicillin 100 U/ml, streptomycin 100 ug/ml). Cells were tested for authenticity by STR at the Hematology Service of the University of Salamanca. NP29 and NP31 cells were obtained from patient samples by Dr. Gabriel Capellá. Cell proliferation experiments were conducted using a Z1 Coulter Particle Counter as described previously [28, 29]. Apoptosis and cell cycle analyses were performed as described [30]. The KRAS mutation status of genomic DNA isolated using TRIzol (Thermo Fisher Scientific) from Capan-1, IMIM-PC1, IMIM-PC2, SKPC1, NP29, and NP31 cell lines was analyzed with the KRAS Mutation Test v2 (LSR) on the Cobas® platform (Roche Diagnostics) by PCR using the Cobas® z 480 analyzer (Roche). The resulting data are presented in Supplementary Table 1.

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In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 4 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.06&#1770.29 nM
Method Description
All cell lines were cultured at 37oC in a humidified atmosphere in the presence of 5% CO2 and 95% air in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% FBS containing high glucose (4500 mg/liter) and antibiotics (penicillin 100 U/ml, streptomycin 100 ug/ml). Cells were tested for authenticity by STR at the Hematology Service of the University of Salamanca. NP29 and NP31 cells were obtained from patient samples by Dr. Gabriel Capellá. Cell proliferation experiments were conducted using a Z1 Coulter Particle Counter as described previously [28, 29]. Apoptosis and cell cycle analyses were performed as described [30]. The KRAS mutation status of genomic DNA isolated using TRIzol (Thermo Fisher Scientific) from Capan-1, IMIM-PC1, IMIM-PC2, SKPC1, NP29, and NP31 cell lines was analyzed with the KRAS Mutation Test v2 (LSR) on the Cobas® platform (Roche Diagnostics) by PCR using the Cobas® z 480 analyzer (Roche). The resulting data are presented in Supplementary Table 1.

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In Vitro Model Pancreatic carcinoma NP31 cells CVCL_E3BS
Experiment 5 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3.83&#1771.91 nM
Method Description
All cell lines were cultured at 37oC in a humidified atmosphere in the presence of 5% CO2 and 95% air in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% FBS containing high glucose (4500 mg/liter) and antibiotics (penicillin 100 U/ml, streptomycin 100 ug/ml). Cells were tested for authenticity by STR at the Hematology Service of the University of Salamanca. NP29 and NP31 cells were obtained from patient samples by Dr. Gabriel Capellá. Cell proliferation experiments were conducted using a Z1 Coulter Particle Counter as described previously [28, 29]. Apoptosis and cell cycle analyses were performed as described [30]. The KRAS mutation status of genomic DNA isolated using TRIzol (Thermo Fisher Scientific) from Capan-1, IMIM-PC1, IMIM-PC2, SKPC1, NP29, and NP31 cell lines was analyzed with the KRAS Mutation Test v2 (LSR) on the Cobas® platform (Roche Diagnostics) by PCR using the Cobas® z 480 analyzer (Roche). The resulting data are presented in Supplementary Table 1.

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In Vitro Model Pancreatic ductal adenocarcinoma IMIM-PC2 cells CVCL_0345
Experiment 6 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
9.17&#1774.23 nM
Method Description
All cell lines were cultured at 37oC in a humidified atmosphere in the presence of 5% CO2 and 95% air in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% FBS containing high glucose (4500 mg/liter) and antibiotics (penicillin 100 U/ml, streptomycin 100 ug/ml). Cells were tested for authenticity by STR at the Hematology Service of the University of Salamanca. NP29 and NP31 cells were obtained from patient samples by Dr. Gabriel Capellá. Cell proliferation experiments were conducted using a Z1 Coulter Particle Counter as described previously [28, 29]. Apoptosis and cell cycle analyses were performed as described [30]. The KRAS mutation status of genomic DNA isolated using TRIzol (Thermo Fisher Scientific) from Capan-1, IMIM-PC1, IMIM-PC2, SKPC1, NP29, and NP31 cell lines was analyzed with the KRAS Mutation Test v2 (LSR) on the Cobas® platform (Roche Diagnostics) by PCR using the Cobas® z 480 analyzer (Roche). The resulting data are presented in Supplementary Table 1.

   Click to Show/Hide
In Vitro Model Pancreatic ductal adenocarcinoma IMIM-PC1 cells CVCL_4061
EP4461318A2 anti-PSMA ADC8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.051 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

   Click to Show/Hide
In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
EP4461318A2 anti-PSMA ADC9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.053 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

   Click to Show/Hide
In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
EP4461318A2 anti-PSMA ADC4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.064 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

   Click to Show/Hide
In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
EP4461318A2 anti-PSMA ADC3 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.066 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

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In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
CN114230664B 353A: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.16 nM
High C10orf54 expression (C10orf54 +++)
Method Description
53A: DBM- (C6)-MMAF was tested in P31/FUJ,100-300nm,3days
In Vitro Model Acute myeloid leukemia, Childhood acute myeloid leukemia P31/FUJ cells CVCL_1632
Experiment 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.34 nM
High C10orf54 expression (C10orf54 +++)
Method Description
53A: DBM- (C6)-MMAF was tested in OCI/AML3,100-300nm,3days
In Vitro Model Adult acute myelomonocytic leukemia, Acute myelomonocytic leukemia OCI/AML3 cells CVCL_1844
Experiment 3 Reporting the Activity Date of This ADC [33]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
4.97 nM
High C10orf54 expression (C10orf54 +++)
Method Description
53A: DBM- (C6)-MMAF was tested in PL21,100-300nm,3days
In Vitro Model Acute promyelocytic leukemia PL21 cells CVCL_2161
EP4461318A2 anti-PSMA ADC12 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.295 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

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In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
EP4461318A2 anti-PSMA ADC7 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.503 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

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In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
EP4461318A2 anti-PSMA ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.543 nM
High FOLH1 expression (FOLH1 +++)
Method Description
In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.

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In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
Anti-CD64 (scFv)-SNAP-Auristatin F [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
14.48 nM
Positive CD64 expression ( CD64+++/++)
Method Description
The therapeutic potential of the CD64-targeting ADC, H22 (scFv)-SNAP-AURIF was investigated using XTT cell viability assays (Sigma-Aldrich, USA). Briefly, 5 × 103 IFN-Gamma stimulated CD64+ U937 cells, CD64- MDA-MB-468 cells or ex vivo differentiated hMDMs were seeded overnight in 96-well plates before treatment with decreasing concentration of H22 (scFv)-SNAP-AURIF or H22 (scFv)-ETA' for 72 h. Thereafter, the treated cells were incubated with freshly prepared XTT labelling reagent (sodium 2,3,-bis (2-methoxy-4-nitro-5-sulfophenyl)-5-[ (phenylamino)-carbonyl]-2H-tetrazolium) and electron coupling reagent mixture, phenanzine methosulfate (50:1) for 4 h. The readout was conducted by measuring absorbance of the reduced XTT reagent at 450 nm with a reference of 655 nm on a Spectrophotometer (Bio-Rad, USA), and the data were analyzed using GraphPad Prism v10.0 software (Graphpad softwares, USA). Data were expressed as mean ± standard error of mean (SEM) unless otherwise indicated.

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In Vitro Model Acute monoblastic/monocytic leukemia, Adult acute monocytic leukemia U937 monocytic cells (IFN-Gamma stimulated) CVCL_0007
aCSPG4 (scFv)-SNAP-AURIF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [37]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
173.3 nM
Method Description
Cells (5 × 103) were seeded in a 96-well plate (in either RPMI-1640 (Gibco #10566) or DMEM medium (Gibco #61870), supplemented with 10% (v/v) heat-inactivated FBS and 1% (v/v) 100 U/mL penicillin-streptomycin) and allowed to adhere overnight under standard tissue culture conditions (37 °C, 5% CO2 and 95% humidity). The next day, they were treated with threefold serially diluted concentrations of MMAF (unmodified), BG-linker-AURIF, alphaCSPG4 (scFv)-SNAP (unconjugated) or alphaCSPG4 (scFv)-SNAP-AURIF and incubated for 72 h in a 5% CO2 incubator with 95% humidity at 37 °C. Untreated cells served as negative controls (100% cell viability), while Zeocin-treated (100 ug/mL) cells were used as positive controls (0% cell viability). The Cell Proliferation Kit II (XTT) (product number: 11465015001, Roche, Switzerland) was used (according to the manufacturer's protocol) to assess cytotoxicity. In this assay, cleavage of the tetrazolium salt XTT occurs in the presence of metabolically active cells and results in the formation of orange formazan crystals, which absorb light at 450 nm. Thus, at 68 h post-treatment, cells were treated with the XTT reagent and at 72 h, absorbance readings (at 450 nm as the measurement filter and 650 nm as the reference filter) were taken using a spectrophotometer (iMarkTM Microplate Absorbance Reader, Bio-Rad, USA). All experiments were carried out in triplicate (n = 3), with 3 technical repeats. The absorbance values were normalized with respect to the untreated and Zeocin controls, and the results were presented as a percentage of cell viability. The concentration required to achieve a 50% reduction in cell viability (IC50 value) was calculated using GraphPad Prism v5 software.

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In Vitro Model Invasive breast carcinoma of no special type Hs578T cells CVCL_0332
Experiment 2 Reporting the Activity Date of This ADC [37]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
190.3 nM
Method Description
Cells (5 × 103) were seeded in a 96-well plate (in either RPMI-1640 (Gibco #10566) or DMEM medium (Gibco #61870), supplemented with 10% (v/v) heat-inactivated FBS and 1% (v/v) 100 U/mL penicillin-streptomycin) and allowed to adhere overnight under standard tissue culture conditions (37 °C, 5% CO2 and 95% humidity). The next day, they were treated with threefold serially diluted concentrations of MMAF (unmodified), BG-linker-AURIF, alphaCSPG4 (scFv)-SNAP (unconjugated) or alphaCSPG4 (scFv)-SNAP-AURIF and incubated for 72 h in a 5% CO2 incubator with 95% humidity at 37 °C. Untreated cells served as negative controls (100% cell viability), while Zeocin-treated (100 ug/mL) cells were used as positive controls (0% cell viability). The Cell Proliferation Kit II (XTT) (product number: 11465015001, Roche, Switzerland) was used (according to the manufacturer's protocol) to assess cytotoxicity. In this assay, cleavage of the tetrazolium salt XTT occurs in the presence of metabolically active cells and results in the formation of orange formazan crystals, which absorb light at 450 nm. Thus, at 68 h post-treatment, cells were treated with the XTT reagent and at 72 h, absorbance readings (at 450 nm as the measurement filter and 650 nm as the reference filter) were taken using a spectrophotometer (iMarkTM Microplate Absorbance Reader, Bio-Rad, USA). All experiments were carried out in triplicate (n = 3), with 3 technical repeats. The absorbance values were normalized with respect to the untreated and Zeocin controls, and the results were presented as a percentage of cell viability. The concentration required to achieve a 50% reduction in cell viability (IC50 value) was calculated using GraphPad Prism v5 software.

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In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [37]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1660 nM
Method Description
Cells (5 × 103) were seeded in a 96-well plate (in either RPMI-1640 (Gibco #10566) or DMEM medium (Gibco #61870), supplemented with 10% (v/v) heat-inactivated FBS and 1% (v/v) 100 U/mL penicillin-streptomycin) and allowed to adhere overnight under standard tissue culture conditions (37 °C, 5% CO2 and 95% humidity). The next day, they were treated with threefold serially diluted concentrations of MMAF (unmodified), BG-linker-AURIF, alphaCSPG4 (scFv)-SNAP (unconjugated) or alphaCSPG4 (scFv)-SNAP-AURIF and incubated for 72 h in a 5% CO2 incubator with 95% humidity at 37 °C. Untreated cells served as negative controls (100% cell viability), while Zeocin-treated (100 ug/mL) cells were used as positive controls (0% cell viability). The Cell Proliferation Kit II (XTT) (product number: 11465015001, Roche, Switzerland) was used (according to the manufacturer's protocol) to assess cytotoxicity. In this assay, cleavage of the tetrazolium salt XTT occurs in the presence of metabolically active cells and results in the formation of orange formazan crystals, which absorb light at 450 nm. Thus, at 68 h post-treatment, cells were treated with the XTT reagent and at 72 h, absorbance readings (at 450 nm as the measurement filter and 650 nm as the reference filter) were taken using a spectrophotometer (iMarkTM Microplate Absorbance Reader, Bio-Rad, USA). All experiments were carried out in triplicate (n = 3), with 3 technical repeats. The absorbance values were normalized with respect to the untreated and Zeocin controls, and the results were presented as a percentage of cell viability. The concentration required to achieve a 50% reduction in cell viability (IC50 value) was calculated using GraphPad Prism v5 software.

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In Vitro Model Cutaneous melanoma SK-MEL-28 cells CVCL_0526
WO2024181570A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [38]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
165 ng/mL
Positive CD138 expression (CD138+++/++)
Method Description
1000 cells/well of Capan-1 in 96 well, 37 °C for 5 days.
In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC [38]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 10000 ng/mL Negative CD138 expression (CD138-)
Method Description
1000 cells/well of Jurkat in 96 well, 37 °C for 5 days.
In Vitro Model T acute lymphoblastic leukemia Jurkat cells CVCL_0065
IN202417078684A+ADC9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [39]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3083 ng/ml
Method Description
The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.
Experiment 2 Reporting the Activity Date of This ADC [39]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
7021 ng/ml
Method Description
The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.
CN114230664B 76E1: DBM- (C6)-MMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [40]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.06 nM
High Nectin-4 expression (Nectin-4 +++)
Method Description
NEC49-9-A was tested in MDA-MB-468,1×106/ml,1h
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [40]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.07 nM
High Nectin-4 expression (Nectin-4 +++)
Method Description
NEC49-9-A was tested in T47D,1×106/ml,1h
In Vitro Model Invasive breast carcinoma of no special type T47D cells CVCL_0553
Experiment 3 Reporting the Activity Date of This ADC [40]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.78 nM
High Nectin-4 expression (Nectin-4 +++)
Method Description
NEC49-9-A was tested in Nectin4-CHOK1,1×106/ml,1h
In Vitro Model Normal CHOK1 cells CVCL_0214
38501590 Anti-HER2 ARC-FDC (2) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.39&#1770.44 nM
High HER2 expression (HER2 +++)
Method Description
Human breast cancer cells in passage 4 or 5 or U937 cells in passage 3 were seeded in 96-well culture plates at a density of 15,000 cells/well in 90 uL culture media. Cells were then treated in duplicates with anti-HER2 ARC-FDCs, anti-HER2 Fab, anti-HER2 Fab-CD38 fusions, or MMAF-alkyne that were prepared in 3-fold serial dilution starting from 300 nM. Cells treated with 5 uM paclitaxel (MilliporeSigma, MA) and PBS were included for 0% and 100% viability controls, respectively. Following incubation at 37°C in an incubator with 5% CO2 for 72 h, cells were added with MTT (3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) reagent (Thermo Fisher Scientific, MA), incubated for 3 h, and lysed with 20% SDS in 50% dimethylformamide. Absorbance at 580 nm was then measured with a Synergy H1 plate reader after 1-hour incubation at 37°C with 5% CO2. EC50 was calculated by the three-parameter nonlinear regression fitting in GraphPad Prism Version 9.4.0 (GraphPad software, CA).

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In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Low HER2 expression (HER2+)
Method Description
Human breast cancer cells in passage 4 or 5 or U937 cells in passage 3 were seeded in 96-well culture plates at a density of 15,000 cells/well in 90 uL culture media. Cells were then treated in duplicates with anti-HER2 ARC-FDCs, anti-HER2 Fab, anti-HER2 Fab-CD38 fusions, or MMAF-alkyne that were prepared in 3-fold serial dilution starting from 300 nM. Cells treated with 5 uM paclitaxel (MilliporeSigma, MA) and PBS were included for 0% and 100% viability controls, respectively. Following incubation at 37°C in an incubator with 5% CO2 for 72 h, cells were added with MTT (3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) reagent (Thermo Fisher Scientific, MA), incubated for 3 h, and lysed with 20% SDS in 50% dimethylformamide. Absorbance at 580 nm was then measured with a Synergy H1 plate reader after 1-hour incubation at 37°C with 5% CO2. EC50 was calculated by the three-parameter nonlinear regression fitting in GraphPad Prism Version 9.4.0 (GraphPad software, CA).

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
38501590 Anti-HER2 ARC-FDC (1) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.3&#1770.37 nM
High HER2 expression (HER2 +++)
Method Description
Human breast cancer cells in passage 4 or 5 or U937 cells in passage 3 were seeded in 96-well culture plates at a density of 15,000 cells/well in 90 uL culture media. Cells were then treated in duplicates with anti-HER2 ARC-FDCs, anti-HER2 Fab, anti-HER2 Fab-CD38 fusions, or MMAF-alkyne that were prepared in 3-fold serial dilution starting from 300 nM. Cells treated with 5 uM paclitaxel (MilliporeSigma, MA) and PBS were included for 0% and 100% viability controls, respectively. Following incubation at 37°C in an incubator with 5% CO2 for 72 h, cells were added with MTT (3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) reagent (Thermo Fisher Scientific, MA), incubated for 3 h, and lysed with 20% SDS in 50% dimethylformamide. Absorbance at 580 nm was then measured with a Synergy H1 plate reader after 1-hour incubation at 37°C with 5% CO2. EC50 was calculated by the three-parameter nonlinear regression fitting in GraphPad Prism Version 9.4.0 (GraphPad software, CA).

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In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Low HER2 expression (HER2+)
Method Description
Human breast cancer cells in passage 4 or 5 or U937 cells in passage 3 were seeded in 96-well culture plates at a density of 15,000 cells/well in 90 uL culture media. Cells were then treated in duplicates with anti-HER2 ARC-FDCs, anti-HER2 Fab, anti-HER2 Fab-CD38 fusions, or MMAF-alkyne that were prepared in 3-fold serial dilution starting from 300 nM. Cells treated with 5 uM paclitaxel (MilliporeSigma, MA) and PBS were included for 0% and 100% viability controls, respectively. Following incubation at 37°C in an incubator with 5% CO2 for 72 h, cells were added with MTT (3- (4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) reagent (Thermo Fisher Scientific, MA), incubated for 3 h, and lysed with 20% SDS in 50% dimethylformamide. Absorbance at 580 nm was then measured with a Synergy H1 plate reader after 1-hour incubation at 37°C with 5% CO2. EC50 was calculated by the three-parameter nonlinear regression fitting in GraphPad Prism Version 9.4.0 (GraphPad software, CA).

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
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