Linker Information
General Information of This Linker
| Linker ID |
LIN0FZQTM
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| Linker Name |
DBCO-Val-Cit-PABC
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C37H42N6O6
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| Isosmiles |
OCC1=CC=C(C=C1)NC([C@@H](NC([C@H](C(C)C)NC(CCC(N2CC3=CC=CC=C3C#CC4=CC=CC=C42)=O)=O)=O)CCCNC(N)=O)=O
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| InChI |
InChI=1S/C37H42N6O6/c1-24(2)34(36(48)41-30(11-7-21-39-37(38)49)35(47)40-29-17-13-25(23-44)14-18-29)42-32(45)19-20-33(46)43-22-28-10-4-3-8-26(28)15-16-27-9-5-6-12-31(27)43/h3-6,8-10,12-14,17-18,24,30,34,44H,7,11,19-23H2,1-2H3,(H,40,47)(H,41,48)(H,42,45)(H3,38,39,49)/t30-,34-/m0/s1
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| InChIKey |
DSBPSTFXGYLDAW-NHZFLZHXSA-N
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| Pharmaceutical Properties |
Molecule Weight
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666.779
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Polar area
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182.96
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Complexity
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1677.467863
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xlogp Value
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2.9183
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Heavy Count
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49
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Rot Bonds
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14
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Hbond acc
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6
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Hbond Donor
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6
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
IN202417103159A 2188-D04-Yl80/F404/K42/E161-LP1 [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) |
0.022 nM
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Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
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| In Vitro Model | Embryonal carcinoma | Ntera-2 cells | CVCL_0034 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Negative ROR1 expression (ROR1-) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A 2188-D04-Yl80/F404/K42-LP1 [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) |
0.082 nM
|
Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
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| In Vitro Model | Embryonal carcinoma | Ntera-2 cells | CVCL_0034 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Negative ROR1 expression (ROR1-) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
IN202417103159A 2188-D04-Yl80/F404-LP1 [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) | > 10 nM | Negative ROR1 expression (ROR1-) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 10 nM | Positive ROR1 expression (ROR1+++/++) | ||
| Method Description |
The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
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| In Vitro Model | Embryonal carcinoma | Ntera-2 cells | CVCL_0034 | ||
References