Payload Information
General Information of This Payload
| Payload ID | PAY0DQMOU |
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|---|---|---|---|---|---|---|
| Name | Mdo-cpt |
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| Synonyms |
Mdo-cpt
Click to Show/Hide
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| Target | DNA topoisomerase I (TOP1) | |||||
| Structure |
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| Formula | C21H16N2O6 |
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| Isosmiles | CC[C@]1(O)C(C=C2C3=NC4=C(C=C3CN52)C=C(OCO6)C6=C4)=C(COC1=O)C5=O |
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| PubChem CID | ||||||
| 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
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| InChIKey |
RPFYDENHBPRCTN-NRFANRHFSA-N
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| Pharmaceutical Properties | Molecule Weight |
392.367 |
Polar area |
99.88 |
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Complexity |
1279.86177 |
xlogp Value |
1.8083 |
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Heavy Count |
29 |
Rot Bonds |
1 |
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Hbond acc |
8 |
Hbond Donor |
1 |
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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
|
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| Half Maximal Inhibitory Concentration (IC50) | 0.043 | ug.mL-1 |
A549 cells
|
Lung adenocarcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 0.05 | ug.mL-1 |
HCT116 cells
|
Colon carcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 0.104 | ug.mL-1 |
HepG2 cells
|
Hepatoblastoma
|
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| Half Maximal Effective Concentration (EC50) | 0.36 | nM |
HCT116 cells
|
Colon carcinoma
|
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| Half Maximal Effective Concentration (EC50) | 0.86 | nM |
A549 cells
|
Lung adenocarcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 0.93 | nM |
SW620 cells
|
Colon adenocarcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
U251 cells
|
Astrocytoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
SN12C cells
|
Renal cell carcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
MOLT-4 cells
|
Adult T acute lymphoblastic leukemia
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
DU145 cells
|
Prostate carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
CCRF-CEM cells
|
T acute lymphoblastic leukemia
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
NCI-H460 cells
|
Lung large cell carcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
786-O cells
|
Renal cell carcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
DMS 114 cells
|
Lung small cell carcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
SF539 cells
|
Gliosarcoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
SF268 cells
|
Astrocytoma
|
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| 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
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
DMS-273 cells
|
Small cell lung carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
HOP-62 cells
|
Non-small cell lung carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
M14 cells
|
Melanoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
SF-295 cells
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Glioblastoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
SR cells
|
Leukemia
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1 | nM |
UACC-62 cells
|
Melanoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.138 | nM |
NCI-H23 cells
|
Lung adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.164 | nM |
UO-31 cells
|
Renal carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.327 | nM |
HL-60 cells
|
Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.33 | nM |
NCI-H522 cells
|
Non-small cell lung carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.355 | nM |
LOX IMVI cells
|
Melanoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.439 | nM |
A549 cells
|
Lung adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.483 | nM |
SNB-75 cells
|
Glioblastoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.524 | nM |
SNB-19 cells
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Astrocytoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.671 | nM |
HCT116 cells
|
Colon carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.679 | nM |
NCI-H226 cells
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Pleural epithelioid mesothelioma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.694 | nM |
SK-MEL-5 cells
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Cutaneous melanoma
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| Half Maximal Growth Inhibitory Concentration (GI50) | 1.734 | nM |
CAKI-1 cells
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Clear cell renal cell carcinoma
|
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| 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
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High grade ovarian serous adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 10 | nM |
MCF-7 cells
|
Invasive breast carcinoma of no special type
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 10.42 | nM |
T47D cells
|
Invasive breast carcinoma of no special type
|
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| Half Maximal Inhibitory Concentration (IC50) | 10.64 | nM |
HepG2 cells
|
Hepatoblastoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 10.67 | nM |
LXFL 529 cells
|
Non-small cell lung carcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 108.57 | nM |
U-87MG ATCC cells
|
Glioblastoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 11.12 | nM |
OVCAR-5 cells
|
Ovarian serous adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 11.8 | nM |
BT-549 cells
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Breast ductal carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 12.11 | nM |
KM-20L2 cells
|
Colon carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 14.29 | nM |
A498 cells
|
Renal carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 14.29 | nM |
RXF 631 cells
|
Renal carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 14.89 | nM |
MDA-MB-435 cells
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Amelanotic melanoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 15.81 | nM |
NCI-H69 cells
|
Lung small cell carcinoma, Small cell lung cancer
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 17.1 | nM |
NCI-H322M cells
|
Minimally invasive lung adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 17.74 | nM |
MDA-N cells
|
Breast carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 18.11 | nM |
HCT-15 cells
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Colon adenocarcinoma
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| Half Maximal Inhibitory Concentration (IC50) | 18.54 | nM |
NCI-H446 cells
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Lung small cell carcinoma
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| Half Maximal Growth Inhibitory Concentration (GI50) | 18.79 | nM |
SK-MEL-28 cells
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Cutaneous melanoma
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| Half Maximal Growth Inhibitory Concentration (GI50) | 2 | nM |
SK-OV-3 cells
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Ovarian serous adenocarcinoma
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| Half Maximal Growth Inhibitory Concentration (GI50) | 2.213 | nM |
RXF 393 cells
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Renal carcinoma
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| 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
|
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| Half Maximal Inhibitory Concentration (IC50) | 21.75 | nM |
Bel-7402 cells
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Hepatoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 22.39 | nM |
SK-MEL-2 cells
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Melanoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 23.5 | nM |
HCT116 cells
|
Colon carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 23.82 | nM |
HCC 2998 cells
|
Colon adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 23.82 | nM |
XF498 cells
|
Glioma
|
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| Half Maximal Inhibitory Concentration (IC50) | 24.19 | nM |
SH-SY5Y cells
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Bone marrow neuroblastoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 243.78 | nM |
Hs578T cells
|
Invasive breast carcinoma of no special type
|
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| Half Maximal Inhibitory Concentration (IC50) | 27 | nM |
HL-60 cells
|
Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 28.05 | nM |
RPMI-8226 cells
|
Plasma cell myeloma
|
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| Half Maximal Inhibitory Concentration (IC50) | 3 | nM |
NCI-H460 cells
|
Lung large cell carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 3.041 | nM |
K562 cells
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Blast phase chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 3.199 | nM |
SW620 cells
|
Colon adenocarcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 30 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 32.2 | nM |
MCF-7 cells
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Invasive breast carcinoma of no special type
|
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| Half Maximal Inhibitory Concentration (IC50) | 32.4 | nM |
HeLa cells
|
Human papillomavirus-related endocervical adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 357.27 | nM |
MDA-MB-231 cells
|
Breast adenocarcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 37.28 | nM |
2008 cells
|
Ovarian carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 375.84 | nM |
SNB-78 cells
|
Glioblastoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 39.5 | nM |
HepG2 cells
|
Hepatoblastoma
|
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| 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
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 4.966 | nM |
Malme-3M cells
|
Melanoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 42.85 | nM |
HOP-18 cells
|
Non-small cell lung adenocarcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 43.85 | nM |
COLO 205 cells
|
Colon adenocarcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 49.66 | nM |
KM12 cells
|
Colon adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 5 | nM |
HCT116 cells
|
Colon carcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 5 | nM |
HCT-8 cells
|
Ileocecal adenocarcinoma
|
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| Half Maximal Effective Concentration (EC50) | 50 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 50.7 | nM |
A549 cells
|
Lung adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 50.7 | nM |
OVCAR-4 cells
|
Ovarian adenocarcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 502.34 | nM |
TK-10 cells
|
Renal carcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 53.95 | nM |
UACC-257 cells
|
Melanoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 55.08 | nM |
OVCAR-3 cells
|
High grade ovarian serous adenocarcinoma
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 55.85 | nM |
DLD-1 cells
|
Colon adenocarcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 6 | nM |
EKVX cells
|
Non-small cell lung carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 6.29 | nM |
H69AR cells
|
Lung small cell carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 6.61 | nM |
NCI-H446 cells
|
Lung small cell carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 63.26 | nM |
MCF-7 cells
|
Invasive breast carcinoma of no special type
|
||
| Half Maximal Growth Inhibitory Concentration (GI50) | 7.464 | nM |
PC-3 cells
|
Prostate carcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 7.87 | nM |
M19-MEL cells
|
Melanoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 78 | nM | Undisclosed | Undisclosed | Undisclosed | |
| Half Maximal Inhibitory Concentration (IC50) | 8.1 | nM |
PC-3 cells
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Prostate carcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 8.87 | nM |
NCI-H446 cells
|
Lung small cell carcinoma
|
||
| Half Maximal Inhibitory Concentration (IC50) | 83 | nM |
A549 cells
|
Lung adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 88.1 | nM |
EKVX cells
|
Non-small cell lung carcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 9 | nM |
A549 cells
|
Lung adenocarcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 9 | nM |
SW620 cells
|
Colon adenocarcinoma
|
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| Half Maximal Growth Inhibitory Concentration (GI50) | 9.484 | nM |
IGROV-1 cells
|
Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma
|
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| Half Maximal Inhibitory Concentration (IC50) | 9.6 | nM |
HeLa cells
|
Human papillomavirus-related endocervical adenocarcinoma
|
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
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
1.0- 9.9 nM
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| 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
|
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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) |
1.0- 9.9 nM
|
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| 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
|
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| 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.
Click to Show/Hide
|
||||
| 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.
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| 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.
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| 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
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| 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
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| In Vitro Model | Breast inflammatory carcinoma | SUM149PT cells (-NE) | CVCL_3422 | ||
WO2024105206A1 23i-5657 2 [Investigative]
Revealed Based on the Cell Line Data
| 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.
Click to Show/Hide
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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.
Click to Show/Hide
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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.
Click to Show/Hide
|
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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.
Click to Show/Hide
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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.
Click to Show/Hide
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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.
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 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
| 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.
Click to Show/Hide
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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
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||||
| 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
| 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
| 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.
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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) (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
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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) |
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
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| 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
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| 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
|
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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 19 % carbon dioxide.
Click to Show/Hide
|
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| 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
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| In Vitro Model | Colon adenocarcinoma | HT29 cells (-NE) | CVCL_0320 | ||
WO2024105206A1 27i-5657 2 [Investigative]
Revealed Based on the Cell Line Data
| 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
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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 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 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.
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) |
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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Breast inflammatory carcinoma | SUM149PT cells (-NE) | CVCL_3422 | ||
WO2024105206A1 32p-Avelu 2 [Investigative]
Revealed Based on the Cell Line Data
| 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.
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 20 % 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 28 % 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 28 % carbon dioxide.
Click to Show/Hide
|
||||
| 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
| 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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Renal cell carcinoma | 786-O cells (-NE) | CVCL_1051 | ||
WO2024105206A1 16i-5657 2 [Investigative]
Revealed Based on the Cell Line Data
| 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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| 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.
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) |
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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| 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.
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) |
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.
Click to Show/Hide
|
||||
| In Vitro Model | Colon adenocarcinoma | HT29 cells (-NE) | CVCL_0320 | ||
