Payload Information

General Information of This Payload

Payload ID	PAY0WDZAK
Name	Auristatin 0101
Synonyms	PF-06380101; 1436391-86-4; Auristatin 0101; Aur0101; Q8020AX34E; AUR-0101; 2-Methyl-L-Alanyl-N-[(3r,4s,5s)-3-Methoxy-1-{(2s)-2-[(1r,2r)-1-Methoxy-2-Methyl-3-Oxo-3-{[(1s)-2-Phenyl-1-(1,3-Thiazol-2-Yl)ethyl]amino}propyl]pyrrolidin-1-Yl}-5-Methyl-1-Oxoheptan-4-Yl]-N-Methyl-L-Valinamide; (2S)-2-((2-Amino-2-methyl-propanoyl)amino)-N-((1S,2R)-2-methoxy-4-((2S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((1S)-2-phenyl-1-thiazol-2-yl-ethyl)amino)propyl)pyrrolidin-1-yl)-1-((1S)-1-methylpropyl)-4-oxo-butyl)-N,3-dimethyl-butanamide; (S)-2-(2-amino-2-methylpropanamido)-N-((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)-N,3-dimethylbutanamide; L-Valinamide, 2-methylalanyl-N-((1S,2R)-2-methoxy-4-((2S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((1S)-2-phenyl-1-(2-thiazolyl)ethyl)amino)propyl)-1-pyrrolidinyl)-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-; Auristatin-0101; UNII-Q8020AX34E; CHEMBL3359827; SCHEMBL14936149; AKOS040742399; CS-3706; NCGC00485972-01; HY-12522; MS-31297; F85106; Q27454197; (2S)-2-[(2-amino-2-methylpropanoyl)amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide; 2-methylalanyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide; 3WD Click to Show/Hide
Target	Microtubule (MT)			Target Info
Structure
Structure	3D MOL		2D MOL
Formula	C39H62N6O6S
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)C3=NC=CS3)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)C(C)(C)N
PubChem CID	71569947
InChI	InChI=1S/C39H62N6O6S/c1-11-25(4)33(44(8)37(48)32(24(2)3)43-38(49)39(6,7)40)30(50-9)23-31(46)45-20-15-18-29(45)34(51-10)26(5)35(47)42-28(36-41-19-21-52-36)22-27-16-13-12-14-17-27/h12-14,16-17,19,21,24-26,28-30,32-34H,11,15,18,20,22-23,40H2,1-10H3,(H,42,47)(H,43,49)/t25-,26+,28-,29-,30+,32-,33-,34+/m0/s1
InChIKey	QAAFNSMAIAVCHE-BZLYQNAUSA-N
IUPAC Name	(2S)-2-[(2-amino-2-methylpropanoyl)amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
Pharmaceutical Properties	Molecule Weight	743	Polar area	184
	Complexity	1170	xlogp Value	4.1
	Heavy Count	52	Rot Bonds	19
	Hbond acc	9	Hbond Donor	3

The activity data of This Payload

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.8	nM	HT-29 cells	Colon adenocarcinoma	CVCL_0320	[1]

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

EDB-ADC [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 6 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 0.75 mg/kg q4dx4.
In Vivo Model	Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 2 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.20%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 1.5 mg/kg q4dx4.
In Vivo Model	Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 3 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.20%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 0.3 mg/kg q4dx4.
In Vivo Model	Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
Experiment 4 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.30%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 1 mg/kg q4dx4.
In Vivo Model	Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)
Experiment 5 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.80%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vivo Model	Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 6 Reporting the Activity Date of This ADC				[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.20%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Mice were treated intravenously every 4 days with phosphate-buffered saline (PBS),Neg-vc0101 (Neg-ADC),EDC-vc0101 (EDB-ADC). This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vivo Model	Nonsmall cell lung cancer PDX model (PDX: PDX-NSX-11122)

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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Athymic nu/nu nude mice were injected subcutaneously in the right flank with 8 10 6 cells suspended in 100% Matrigel. This tumor model was injected intravenously with EDB-ADC 1 mg/kg q4dx4.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.10%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Athymic nu/nu nude mice were injected subcutaneously in the right flank with 8 10 6 cells suspended in 100% Matrigel. This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High FN1 expression (FN1+++)
Method Description	EDB+FN expression was evaluated in NSCLC and pancreatic cancer xenografts in immunocompromised mice using IHC. Athymic nu/nu nude mice were injected subcutaneously in the right flank with 8 10 6 cells suspended in 100% Matrigel. This tumor model was injected intravenously with EDB-ADC 3 mg/kg q4dx4.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Anti-IL13RA2-ADC [Investigative]

ADC Info

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					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 29.60%	High IL13RA2 expression (IL13RA2+++)
Method Description	2 x10⁶ A375 cells in 50% Cultrex basement membrane extract were injected subcutaneously in the flank of athymic nu/nu mice for FMT imaging or in the upper right shoulder for PET/CT imaging.
In Vivo Model	A375 xenograft model
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132

3G10-TG6-vc0101 [Investigative]

ADC Info

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					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 1.5 mg/kg.
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.80%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 1.5 mg/kg.
In Vivo Model	HPB-ALL CDX model
In Vitro Model	T acute lymphoblastic leukemia	HPB-ALL cells		CVCL_1820
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.90%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 3 mg/kg.
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 3 mg/kg.
In Vivo Model	HPB-ALL CDX model
In Vitro Model	T acute lymphoblastic leukemia	HPB-ALL cells		CVCL_1820
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 6 mg/kg.
In Vivo Model	HPB-ALL CDX model
In Vitro Model	T acute lymphoblastic leukemia	HPB-ALL cells		CVCL_1820
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 6 mg/kg.
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 6 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	T acute lymphoblastic leukemia	HPB-ALL cells		CVCL_1820
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Plasma cell myeloma	RPMI-8226 cells		CVCL_0014
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.86 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.53 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792

6B6-TG6-vc0101 [Investigative]

ADC Info

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)	≈ 67.90%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 1.5 mg/kg.
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.70%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 3 mg/kg.
In Vivo Model	Ramos CDX model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Mice were treated with a single intravenous dose of the ADCs at 6 mg/kg.
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 6 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 CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	T acute lymphoblastic leukemia	HPB-ALL cells		CVCL_1820
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Plasma cell myeloma	RPMI-8226 cells		CVCL_0014
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.56 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CXCR4 expression (CXCR4+++/++)
Method Description	Cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

RcEDB-ADC [Investigative]

ADC Info

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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.70%	High FN1 expression (FN1+++)
Method Description	For studies using the mouse syngeneic cell line EMT6, 8-week-old Balb/c mice were injected in the left mammary fat pad with 1 x10⁶ cells suspended in DPBS. Tumors were measured at least twice/week. This tumor model was injected intravenously with rcEDB-ADC 1.5 mg/kg q4dx3.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.70%	High FN1 expression (FN1+++)
Method Description	For studies using the mouse syngeneic cell line EMT6, 8-week-old Balb/c mice were injected in the left mammary fat pad with 1 x10⁶ cells suspended in DPBS. Tumors were measured at least twice/week. This tumor model was injected intravenously with rcEDB-ADC 3 mg/kg q4dx3.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.70%	High FN1 expression (FN1+++)
Method Description	For studies using the mouse syngeneic cell line EMT6, 8-week-old Balb/c mice were injected in the left mammary fat pad with 1 x10⁶ cells suspended in DPBS. Tumors were measured at least twice/week. This tumor model was injected intravenously with rcEDB-ADC 9 mg/kg single.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.30%	High FN1 expression (FN1+++)
Method Description	For studies using the mouse syngeneic cell line EMT6, 8-week-old Balb/c mice were injected in the left mammary fat pad with 1 x10⁶ cells suspended in DPBS. Tumors were measured at least twice/week. This tumor model was injected intravenously with rcEDB-ADC 4.5 mg/kg q4dx2.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923

Anti-CXCR4 ADC 381 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Anti-CXCR4 ADC 519 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Anti-CXCR4 ADC 518 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Anti-CXCR4 ADC 554 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.5 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Anti-CXCR4 ADC 553 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.1 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Anti-CXCR4 ADC 555 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.7 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Anti-MSL1 mAb-Compound 31 [Investigative]

ADC Info

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)	37.38 nM	Positive MSL expression (MSL+++/++)
Method Description	The cells were incubated in a CO₂ incubat or with saturated water overnight, On the second day, two covalent thiol conjugated ADCs were serially diluted conjugates were added to the 96 well plate containing OVCAR3 cells, 100uL per well. The initial conjugate was 100000 ng/ml and diluted to 0.001 ng/ml. OVCAR3 cells with added ADC were incubated at 37 for 72 hours. Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Anti-CXCR4 ADC 556 [Investigative]

ADC Info

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					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.7 nM	High CXCR4 expression (CXCR4+++)
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	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

EDB-L19-vc-0101 [Investigative]

ADC Info

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					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	184 ng/mL	Positive EDB expression (EDB+++/++)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Normal	WI38-VA13 cells		CVCL_2759
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15346 ng/mL	Negative EDB expression (EDB-)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

EDB- (K94R)-vc-0101 [Investigative]

ADC Info

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					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	184 ng/mL	Positive EDB expression (EDB+++/++)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Normal	WI38-VA13 cells		CVCL_2759
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10577 ng/mL	Negative EDB expression (EDB-)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

EDB- (κK183C-K290C)-vc-0101 [Investigative]

ADC Info

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					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	198 ng/mL	Positive EDB expression (EDB+++/++)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Normal	WI38-VA13 cells		CVCL_2759
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9276 ng/mL	Negative EDB expression (EDB-)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

EDB- (κK183C-K94R-K290C)-vc-0101 [Investigative]

ADC Info

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					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	216 ng/mL	Positive EDB expression (EDB+++/++)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Normal	WI38-VA13 cells		CVCL_2759
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15584 ng/mL	Negative EDB expression (EDB-)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

References

Ref 1	Cytotoxic Barrigenol-like Triterpenoids from an Extract of Cyrilla racemiflora Housed in a Repository. J Nat Prod. 2015 Oct 23;78(10):2440-6. doi: 10.1021/acs.jnatprod.5b00532. Epub 2015 Sep 30.
Ref 2	Anti-Extra Domain B Splice Variant of Fibronectin Antibody-Drug Conjugate Eliminates Tumors with Enhanced Efficacy When Combined with Checkpoint Blockade. Mol Cancer Ther. 2022 Sep 6;21(9):1462-1472.
Ref 3	Targeting and pharmacology of an anti-IL13R2 antibody and antibody-drug conjugate in a melanoma xenograft model. MAbs. 2021 Jan-Dec;13(1):1958662.
Ref 4	Anti-cxcr4 antibodies and antibody-drug conjugates.
Ref 5	Optimal design, anti-tumour efficacy and tolerability of anti-CXCR4 antibody drug conjugates. Sci Rep. 2019 Feb 21;9(1):2443. doi: 10.1038/s41598-019-38745-x.
Ref 6	Covalent linkers in antibody-drug conjugates and methods of making and using the same.
Ref 7	Anti-EDB antibodies and antibody-drug conjugates

Payload Information

Citation

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)