Payload Information
General Information of This Payload
| Payload ID | PAY0GFWCQ |
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| Name | DM21-C |
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| Synonyms |
DM21-C
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| Target(s) | Microtubule (MT) | |||||
| Structure |
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| Formula | C38H54ClN3O10S |
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| Isosmiles | COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCCCCS)[C@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)C(OC)/C=C/C=C(\C)C2 |
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| InChI |
InChI=1S/C38H54ClN3O10S/c1-22-13-12-14-29(49-8)38(47)21-28(50-36(46)40-38)23(2)34-37(4,52-34)30(51-35(45)24(3)41(5)31(43)15-10-9-11-16-53)20-32(44)42(6)26-18-25(17-22)19-27(48-7)33(26)39/h12-14,18-19,23-24,28-30,34,47,53H,9-11,15-17,20-21H2,1-8H3,(H,40,46)/b14-12+,22-13+/t23-,24+,28+,29?,30+,34+,37+,38+/m1/s1
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| InChIKey |
VNWBDUCJQWNNMQ-UPTSXCKISA-N
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| Pharmaceutical Properties | Molecule Weight |
780.381 |
Polar area |
156.47 |
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Complexity |
779.3218436 |
xlogp Value |
5.0047 |
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Heavy Count |
53 |
Rot Bonds |
10 |
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Hbond acc |
11 |
Hbond Donor |
3 |
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The activity data of This Payload
| Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
|---|---|---|---|---|---|---|
| Inhibition rate | ≈10.3 | % |
SUN-5 cells
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Gastric carcinoma
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Undisclosed | [1] |
| Inhibition rate | ≈12.2 | % |
HPAF-II cells
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Pancreatic ductal adenocarcinoma
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[1] | |
| Inhibition rate | ≈49.5 | % |
MDA-MB-468 cells
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Breast adenocarcinoma
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[1] | |
| Inhibition rate | ≈69.4 | % |
BT-20 cells
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Invasive breast carcinoma of no special type
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[1] |
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
IMGC-936 [Phase 1/2]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04622774 | Phase Status | Phase 1 | ||
| Clinical Description |
A phase 1/2, first-in-human, open-label, dose-escalation and expansion study of IMGC936 (Anti-ADAM9 antibody drug conjugate) in patients with advanced solid tumors.
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| Primary Endpoint |
During dose escalation measure incidence and severity of Treatment Emergent Adverse Events, During dose escalation characterize dose-limiting toxicities (DLTs), During expansion describe the overall response rate.
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| Other Endpoint |
During dose escalation and expansion to characterize study drug concentration and the concentration of anti-drug antibody, During dose expansion describe the duration of response and progression free survival, During dose escalation to describe the objective response rate and duration of response, During dose expansion measure incidence and severity of Treatment Emergent Adverse Events.
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IMGN151 [Phase 1]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
100.00%
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High FOLR1 expression (FOLR1+++; IHC H-score=300) | ||
| Method Description |
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
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| In Vivo Model | KB CDX model | ||||
| In Vitro Model | Human papillomavirus-related endocervical adenocarcinoma | KB cells | CVCL_0372 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
100.00%
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Moderate FOLR1 expression (FOLR1++; IHC H-score=140) | ||
| Method Description |
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
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| In Vivo Model | IGROV-1 CDX model | ||||
| In Vitro Model | Ovarian endometrioid adenocarcinoma | IGROV-1 cells | CVCL_1304 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
100.00%
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Moderate FOLR1 expression (FOLR1++; IHC H-score=100) | ||
| Method Description |
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
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| In Vivo Model | Ishikawa CDX model | ||||
| In Vitro Model | Endometrial adenocarcinoma | Ishikawa cells | CVCL_2529 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
100.00%
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Low FOLR1 expression (FOLR1+; IHC H-score=30) | ||
| Method Description |
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
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| In Vivo Model | OV-90 CDX model | ||||
| In Vitro Model | Ovarian adenocarcinoma | OV-90 cells | CVCL_3768 | ||
References