Payload Information
General Information of This Payload
| Payload ID | PAY0QYSVZ |
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|---|---|---|---|---|---|---|
| Name | Cryptophycin-uD[Dap (Me)] |
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| Synonyms |
Cp; cryptophycin-uD[Dap (Me)]
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| Target | Microtubule (MT) | |||||
| Formula | C34H43ClN4O7 |
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| Isosmiles | C[C@@H](C(OC([C@@H]1CNC)=O)C/C=C/C(N[C@@H](C(NCC(C)(C)C(N1)=O)=O)CC2=CC=C(OC)C(Cl)=C2)=O)[C@@H]3[C@H](O3)C4=CC=CC=C4 |
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| InChI |
InChI=1S/C34H43ClN4O7/c1-20(29-30(46-29)22-10-7-6-8-11-22)26-12-9-13-28(40)38-24(17-21-14-15-27(44-5)23(35)16-21)31(41)37-19-34(2,3)33(43)39-25(18-36-4)32(42)45-26/h6-11,13-16,20,24-26,29-30,36H,12,17-19H2,1-5H3,(H,37,41)(H,38,40)(H,39,43)/t20-,24+,25-,26?,29+,30+/m0/s1
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| InChIKey |
UMJLNORFEWVDQP-RKNORIPQSA-N
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| Pharmaceutical Properties | Molecule Weight |
655.192 |
Polar area |
147.39 |
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Complexity |
1380.371606 |
xlogp Value |
2.8704 |
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Heavy Count |
46 |
Rot Bonds |
8 |
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Hbond acc |
8 |
Hbond Donor |
4 |
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Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Tras (C8)-Cp [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
24ۮ pM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
115䕔 pM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
732𫐿 pM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Bladder carcinoma | RT112 cells | CVCL_1670 | ||
Tras (C4)-Cp [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
30 pM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
515𫐫 pM
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Moderate HER2 expression (HER2++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Bladder carcinoma | RT112 cells | CVCL_1670 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
982𫛫 pM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Tras (C2)-Cp [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
59䔮 pM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
1208𫔬 pM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
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| In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
References