General Information of This Payload
Payload ID
PAY0DQMOU
Name
Mdo-cpt
Synonyms
Mdo-cpt
   Click to Show/Hide
Target DNA topoisomerase I (TOP1)
Structure
Formula
C21H16N2O6
Isosmiles
CC[C@]1(O)C(C=C2C3=NC4=C(C=C3CN52)C=C(OCO6)C6=C4)=C(COC1=O)C5=O
PubChem CID
72403
InChI
InChI=1S/C21H16N2O6/c1-2-21(26)13-5-15-18-11(7-23(15)19(24)12(13)8-27-20(21)25)3-10-4-16-17(29-9-28-16)6-14(10)22-18/h3-6,26H,2,7-9H2,1H3/t21-/m0/s1
InChIKey
RPFYDENHBPRCTN-NRFANRHFSA-N
Pharmaceutical Properties
Molecule Weight
392.367
Polar area
99.88
Complexity
1279.86177
xlogp Value
1.8083
Heavy Count
29
Rot Bonds
1
Hbond acc
8
Hbond Donor
1
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 0.04 ug.mL-1
HeLa cells
Human papillomavirus-related endocervical adenocarcinoma
CVCL_0030 
Half Maximal Inhibitory Concentration (IC50) 0.043 ug.mL-1
A549 cells
Lung adenocarcinoma
CVCL_0023 
Half Maximal Inhibitory Concentration (IC50) 0.05 ug.mL-1
HCT116 cells
Colon carcinoma
CVCL_0291 
Half Maximal Inhibitory Concentration (IC50) 0.104 ug.mL-1
HepG2 cells
Hepatoblastoma
CVCL_0027 
Half Maximal Effective Concentration (EC50) 0.36 nM
HCT116 cells
Colon carcinoma
CVCL_0291 
Half Maximal Effective Concentration (EC50) 0.86 nM
A549 cells
Lung adenocarcinoma
CVCL_0023 
Half Maximal Inhibitory Concentration (IC50) 0.93 nM
SW620 cells
Colon adenocarcinoma
CVCL_0547 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
U251 cells
Astrocytoma
CVCL_0021 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
SN12C cells
Renal cell carcinoma
CVCL_1705 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
MOLT-4 cells
Adult T acute lymphoblastic leukemia
CVCL_0013 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
DU145 cells
Prostate carcinoma
CVCL_0105 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
CCRF-CEM cells
T acute lymphoblastic leukemia
CVCL_0207 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
NCI-H460 cells
Lung large cell carcinoma
CVCL_0459 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
786-O cells
Renal cell carcinoma
CVCL_1051 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
DMS 114 cells
Lung small cell carcinoma
CVCL_1174 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
SF539 cells
Gliosarcoma
CVCL_1691 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
SF268 cells
Astrocytoma
CVCL_1689 
Half Maximal Effective Concentration (EC50) 1 nM
NSCLC cells
Multiple myeloma, Plasma cell myeloma
Undisclosed
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
ACHN cells
Renal adenocarcinoma
CVCL_1067 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
DMS-273 cells
Small cell lung carcinoma
CVCL_1176 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
HOP-62 cells
Non-small cell lung carcinoma
CVCL_1285 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
M14 cells
Melanoma
CVCL_1395 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
SF-295 cells
Glioblastoma
CVCL_1690 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
SR cells
Leukemia
CVCL_1711 
Half Maximal Growth Inhibitory Concentration (GI50) 1 nM
UACC-62 cells
Melanoma
CVCL_1780 
Half Maximal Growth Inhibitory Concentration (GI50) 1.138 nM
NCI-H23 cells
Lung adenocarcinoma
CVCL_1547 
Half Maximal Growth Inhibitory Concentration (GI50) 1.164 nM
UO-31 cells
Renal carcinoma
CVCL_1911 
Half Maximal Growth Inhibitory Concentration (GI50) 1.327 nM
HL-60 cells
Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation
CVCL_0002 
Half Maximal Growth Inhibitory Concentration (GI50) 1.33 nM
NCI-H522 cells
Non-small cell lung carcinoma
CVCL_1567 
Half Maximal Growth Inhibitory Concentration (GI50) 1.355 nM
LOX IMVI cells
Melanoma
CVCL_1381 
Half Maximal Growth Inhibitory Concentration (GI50) 1.439 nM
A549 cells
Lung adenocarcinoma
CVCL_0023 
Half Maximal Growth Inhibitory Concentration (GI50) 1.483 nM
SNB-75 cells
Glioblastoma
CVCL_1706 
Half Maximal Growth Inhibitory Concentration (GI50) 1.524 nM
SNB-19 cells
Astrocytoma
CVCL_0535 
Half Maximal Growth Inhibitory Concentration (GI50) 1.671 nM
HCT116 cells
Colon carcinoma
CVCL_0291 
Half Maximal Growth Inhibitory Concentration (GI50) 1.679 nM
NCI-H226 cells
Pleural epithelioid mesothelioma
CVCL_1544 
Half Maximal Growth Inhibitory Concentration (GI50) 1.694 nM
SK-MEL-5 cells
Cutaneous melanoma
CVCL_0527 
Half Maximal Growth Inhibitory Concentration (GI50) 1.734 nM
CAKI-1 cells
Clear cell renal cell carcinoma
CVCL_0234 
Half Maximal Growth Inhibitory Concentration (GI50) 1.75 nM
Cancer cells
Multiple myeloma, Plasma cell myeloma
Undisclosed
Half Maximal Growth Inhibitory Concentration (GI50) 1.888 nM
OVCAR-8 cells
High grade ovarian serous adenocarcinoma
CVCL_1629 
Half Maximal Growth Inhibitory Concentration (GI50) 10 nM
MCF-7 cells
Invasive breast carcinoma of no special type
CVCL_0031 
Half Maximal Growth Inhibitory Concentration (GI50) 10.42 nM
T47D cells
Invasive breast carcinoma of no special type
CVCL_0553 
Half Maximal Inhibitory Concentration (IC50) 10.64 nM
HepG2 cells
Hepatoblastoma
CVCL_0027 
Half Maximal Growth Inhibitory Concentration (GI50) 10.67 nM
LXFL 529 cells
Non-small cell lung carcinoma
CVCL_D085 
Half Maximal Inhibitory Concentration (IC50) 108.57 nM
U-87MG ATCC cells
Glioblastoma
CVCL_0022 
Half Maximal Growth Inhibitory Concentration (GI50) 11.12 nM
OVCAR-5 cells
Ovarian serous adenocarcinoma
CVCL_1628 
Half Maximal Growth Inhibitory Concentration (GI50) 11.8 nM
BT-549 cells
Breast ductal carcinoma
CVCL_1092 
Half Maximal Growth Inhibitory Concentration (GI50) 12.11 nM
KM-20L2 cells
Colon carcinoma
CVCL_D889 
Half Maximal Growth Inhibitory Concentration (GI50) 14.29 nM
A498 cells
Renal carcinoma
CVCL_1056 
Half Maximal Growth Inhibitory Concentration (GI50) 14.29 nM
RXF 631 cells
Renal carcinoma
CVCL_A780 
Half Maximal Growth Inhibitory Concentration (GI50) 14.89 nM
MDA-MB-435 cells
Amelanotic melanoma
CVCL_0417 
Half Maximal Inhibitory Concentration (IC50) 15.81 nM
NCI-H69 cells
Lung small cell carcinoma, Small cell lung cancer
CVCL_1579 
Half Maximal Growth Inhibitory Concentration (GI50) 17.1 nM
NCI-H322M cells
Minimally invasive lung adenocarcinoma
CVCL_1557 
Half Maximal Growth Inhibitory Concentration (GI50) 17.74 nM
MDA-N cells
Breast carcinoma
CVCL_1910 
Half Maximal Growth Inhibitory Concentration (GI50) 18.11 nM
HCT-15 cells
Colon adenocarcinoma
CVCL_0292 
Half Maximal Inhibitory Concentration (IC50) 18.54 nM
NCI-H446 cells
Lung small cell carcinoma
CVCL_1562 
Half Maximal Growth Inhibitory Concentration (GI50) 18.79 nM
SK-MEL-28 cells
Cutaneous melanoma
CVCL_0526 
Half Maximal Growth Inhibitory Concentration (GI50) 2 nM
SK-OV-3 cells
Ovarian serous adenocarcinoma
CVCL_0532 
Half Maximal Growth Inhibitory Concentration (GI50) 2.213 nM
RXF 393 cells
Renal carcinoma
CVCL_1673 
Half Maximal Effective Concentration (EC50) 2.28 nM
Cancer cells
Multiple myeloma, Plasma cell myeloma
Undisclosed
Half Maximal Growth Inhibitory Concentration (GI50) 2.6 nM
HOP-92 cells
Non-small cell lung carcinoma
CVCL_1286 
Half Maximal Inhibitory Concentration (IC50) 21.75 nM
Bel-7402 cells
Hepatoma
CVCL_5492 
Half Maximal Growth Inhibitory Concentration (GI50) 22.39 nM
SK-MEL-2 cells
Melanoma
CVCL_0069 
Half Maximal Inhibitory Concentration (IC50) 23.5 nM
HCT116 cells
Colon carcinoma
CVCL_0291 
Half Maximal Growth Inhibitory Concentration (GI50) 23.82 nM
HCC 2998 cells
Colon adenocarcinoma
CVCL_1266 
Half Maximal Growth Inhibitory Concentration (GI50) 23.82 nM
XF498 cells
Glioma
CVCL_8928 
Half Maximal Inhibitory Concentration (IC50) 24.19 nM
SH-SY5Y cells
Bone marrow neuroblastoma
CVCL_0019 
Half Maximal Growth Inhibitory Concentration (GI50) 243.78 nM
Hs578T cells
Invasive breast carcinoma of no special type
CVCL_0332 
Half Maximal Inhibitory Concentration (IC50) 27 nM
HL-60 cells
Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation
CVCL_0002 
Half Maximal Growth Inhibitory Concentration (GI50) 28.05 nM
RPMI-8226 cells
Plasma cell myeloma
CVCL_0014 
Half Maximal Inhibitory Concentration (IC50) 3 nM
NCI-H460 cells
Lung large cell carcinoma
CVCL_0459 
Half Maximal Growth Inhibitory Concentration (GI50) 3.041 nM
K562 cells
Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia
CVCL_0004 
Half Maximal Growth Inhibitory Concentration (GI50) 3.199 nM
SW620 cells
Colon adenocarcinoma
CVCL_0547 
Half Maximal Inhibitory Concentration (IC50) 30 nM Undisclosed Undisclosed Undisclosed
Half Maximal Inhibitory Concentration (IC50) 32.2 nM
MCF-7 cells
Invasive breast carcinoma of no special type
CVCL_0031 
Half Maximal Inhibitory Concentration (IC50) 32.4 nM
HeLa cells
Human papillomavirus-related endocervical adenocarcinoma
CVCL_0030 
Half Maximal Growth Inhibitory Concentration (GI50) 357.27 nM
MDA-MB-231 cells
Breast adenocarcinoma
CVCL_0062 
Half Maximal Inhibitory Concentration (IC50) 37.28 nM
2008 cells
Ovarian carcinoma
CVCL_0473 
Half Maximal Growth Inhibitory Concentration (GI50) 375.84 nM
SNB-78 cells
Glioblastoma
CVCL_B321 
Half Maximal Inhibitory Concentration (IC50) 39.5 nM
HepG2 cells
Hepatoblastoma
CVCL_0027 
Half Maximal Effective Concentration (EC50) 4.14 nM
Cancer cells
Multiple myeloma, Plasma cell myeloma
Undisclosed
Half Maximal Growth Inhibitory Concentration (GI50) 4.721 nM
HT-29 cells
Colon adenocarcinoma
CVCL_0320 
Half Maximal Growth Inhibitory Concentration (GI50) 4.966 nM
Malme-3M cells
Melanoma
CVCL_1438 
Half Maximal Growth Inhibitory Concentration (GI50) 42.85 nM
HOP-18 cells
Non-small cell lung adenocarcinoma
CVCL_H642 
Half Maximal Growth Inhibitory Concentration (GI50) 43.85 nM
COLO 205 cells
Colon adenocarcinoma
CVCL_0218 
Half Maximal Growth Inhibitory Concentration (GI50) 49.66 nM
KM12 cells
Colon adenocarcinoma
CVCL_1331 
Half Maximal Inhibitory Concentration (IC50) 5 nM
HCT116 cells
Colon carcinoma
CVCL_0291 
Half Maximal Inhibitory Concentration (IC50) 5 nM
HCT-8 cells
Ileocecal adenocarcinoma
CVCL_2478 
Half Maximal Effective Concentration (EC50) 50 nM Undisclosed Undisclosed Undisclosed
Half Maximal Inhibitory Concentration (IC50) 50.7 nM
A549 cells
Lung adenocarcinoma
CVCL_0023 
Half Maximal Growth Inhibitory Concentration (GI50) 50.7 nM
OVCAR-4 cells
Ovarian adenocarcinoma
CVCL_1627 
Half Maximal Growth Inhibitory Concentration (GI50) 502.34 nM
TK-10 cells
Renal carcinoma
CVCL_1773 
Half Maximal Growth Inhibitory Concentration (GI50) 53.95 nM
UACC-257 cells
Melanoma
CVCL_1779 
Half Maximal Growth Inhibitory Concentration (GI50) 55.08 nM
OVCAR-3 cells
High grade ovarian serous adenocarcinoma
CVCL_0465 
Half Maximal Growth Inhibitory Concentration (GI50) 55.85 nM
DLD-1 cells
Colon adenocarcinoma
CVCL_0248 
Half Maximal Inhibitory Concentration (IC50) 6 nM
EKVX cells
Non-small cell lung carcinoma
CVCL_1195 
Half Maximal Inhibitory Concentration (IC50) 6.29 nM
H69AR cells
Lung small cell carcinoma
CVCL_3513 
Half Maximal Inhibitory Concentration (IC50) 6.61 nM
NCI-H446 cells
Lung small cell carcinoma
CVCL_1562 
Half Maximal Inhibitory Concentration (IC50) 63.26 nM
MCF-7 cells
Invasive breast carcinoma of no special type
CVCL_0031 
Half Maximal Growth Inhibitory Concentration (GI50) 7.464 nM
PC-3 cells
Prostate carcinoma
CVCL_0035 
Half Maximal Growth Inhibitory Concentration (GI50) 7.87 nM
M19-MEL cells
Melanoma
CVCL_B415 
Half Maximal Inhibitory Concentration (IC50) 78 nM Undisclosed Undisclosed Undisclosed
Half Maximal Inhibitory Concentration (IC50) 8.1 nM
PC-3 cells
Prostate carcinoma
CVCL_0035 
Half Maximal Inhibitory Concentration (IC50) 8.87 nM
NCI-H446 cells
Lung small cell carcinoma
CVCL_1562 
Half Maximal Inhibitory Concentration (IC50) 83 nM
A549 cells
Lung adenocarcinoma
CVCL_0023 
Half Maximal Growth Inhibitory Concentration (GI50) 88.1 nM
EKVX cells
Non-small cell lung carcinoma
CVCL_1195 
Half Maximal Inhibitory Concentration (IC50) 9 nM
A549 cells
Lung adenocarcinoma
CVCL_0023 
Half Maximal Inhibitory Concentration (IC50) 9 nM
SW620 cells
Colon adenocarcinoma
CVCL_0547 
Half Maximal Growth Inhibitory Concentration (GI50) 9.484 nM
IGROV-1 cells
Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma
CVCL_1304 
Half Maximal Inhibitory Concentration (IC50) 9.6 nM
HeLa cells
Human papillomavirus-related endocervical adenocarcinoma
CVCL_0030 
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
WO2024105206A1 19i-5657 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 6 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 7 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 6 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 7 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 8 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 8 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 26 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.

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In Vitro Model Breast inflammatory carcinoma SUM149PT cells (+NE) CVCL_3422
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 29 % carbon dioxide.

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In Vitro Model Colon adenocarcinoma HT29 cells (+NE) CVCL_0320
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 26 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 9 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Colon adenocarcinoma HT29 cells (-NE) CVCL_0320
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Breast inflammatory carcinoma SUM149PT cells (-NE) CVCL_3422
WO2024105206A1 23i-5657 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 10 % carbon dioxide.

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In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 10 % carbon dioxide.

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In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 18 % carbon dioxide.

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In Vitro Model Breast inflammatory carcinoma SUM149PT cells (+NE) CVCL_3422
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 28 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 18 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 28 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 18 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 18 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Breast inflammatory carcinoma SUM149PT cells (-NE) CVCL_3422
WO2024105206A1 28i-5657 2 [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 [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 16 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 16 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 30 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 24 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 24 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Breast inflammatory carcinoma SUM149PT cells (+NE) CVCL_3422
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 33 % carbon dioxide.

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In Vitro Model Colon adenocarcinoma HT29 cells (+NE) CVCL_0320
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 30 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 13 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Colon adenocarcinoma HT29 cells (-NE) CVCL_0320
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 24 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 24 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Breast inflammatory carcinoma SUM149PT cells (-NE) CVCL_3422
WO2024105206A1 29p-Avelu 2 [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 [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 17 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 17 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 25 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 25 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
WO2024105206A1 23p-Avelu 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 11 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 11 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 29 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 19 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 32 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Colon adenocarcinoma HT29 cells (+NE) CVCL_0320
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 29 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 19 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
100- 999 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 12 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Colon adenocarcinoma HT29 cells (-NE) CVCL_0320
WO2024105206A1 27i-5657 2 [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 [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.

   Click to Show/Hide
In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.

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In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 23 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 23 % carbon dioxide.

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In Vitro Model Breast inflammatory carcinoma SUM149PT cells (+NE) CVCL_3422
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 23 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 23 % carbon dioxide.

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In Vitro Model Breast inflammatory carcinoma SUM149PT cells (-NE) CVCL_3422
WO2024105206A1 32p-Avelu 2 [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 [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 20 % carbon dioxide.

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In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (-NE) CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 20 % carbon dioxide.

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In Vitro Model Lung small cell carcinoma, Small cell lung cancer NCI-H69 cells (+NE) CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 28 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 28 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
wO2024105206A1 8i-5657 [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 [1]
Efficacy Data Activity Concentration at -50% (AC50)
0.01- 1 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 19 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 19 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
WO2024105206A1 16i-5657 2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 12 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (+NE) CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
1.0- 9.9 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 12 % carbon dioxide.

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In Vitro Model Breast inflammatory carcinoma SUM149PT cells (+NE) CVCL_3422
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 23 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (+NE) CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 26 % carbon dioxide.

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In Vitro Model Colon adenocarcinoma HT29 cells (+NE) CVCL_0320
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 12 % carbon dioxide.

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In Vitro Model Plasma cell myeloma, Multiple myeloma NCI-H929 cells (-NE) CVCL_1600
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
10- 99 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (SUM149PT 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 12 % carbon dioxide.

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In Vitro Model Breast inflammatory carcinoma SUM149PT cells (-NE) CVCL_3422
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
100- 999 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 23 % carbon dioxide.

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In Vitro Model Renal cell carcinoma 786-O cells (-NE) CVCL_1051
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Activity Concentration at -50% (AC50)
100- 999 nM
Method Description
After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 6 % carbon dioxide.

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In Vitro Model Colon adenocarcinoma HT29 cells (-NE) CVCL_0320
References
Ref 1 Antibody-drug conjugates cleavable in a tumor microenvironment