Linker Information
General Information of This Linker
| Linker ID |
LIN0UNSGO
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| Linker Name |
WO2024239281A1, C207, Linker
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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 |
C90H142N16O40
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| Isosmiles |
CC([C@H](NC([C@@H](NC(CCCNC(C(C(N(C(C=C1)=O)C1=O)C(NCCCC(N[C@H](C(N[C@@H](C(C)C)C(N[C@@H](C)C(O)=O)=O)=O)CCCCNC(OCCOCCOCCOCCCCNC(CC[C@H](C(O)=O)N[C@H](C(O)=O)CCC(O)=O)=O)=O)=O)=O)N(C(C=C2)=O)C2=O)=O)=O)CCCCNC(OCCOCCOCCOCCCCNC(CC[C@@H](C(O)=O)N[C@H](C(O)=O)CCC(O)=O)=O)=O)=O)C(N[C@@H](C)C(O)=O)=O)C
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| InChI |
InChI=1S/C90H142N16O40/c1-53(2)73(79(121)97-55(5)83(125)126)103-77(119)57(17-7-9-35-95-89(137)145-51-49-143-47-45-141-43-41-139-39-13-11-33-91-63(107)25-21-59(85(129)130)99-61(87(133)134)23-31-71(115)116)101-65(109)19-15-37-93-81(123)75(105-67(111)27-28-68(105)112)76(106-69(113)29-30-70(106)114)82(124)94-38-16-20-66(110)102-58(78(120)104-74(54(3)4)80(122)98-56(6)84(127)128)18-8-10-36-96-90(138)146-52-50-144-48-46-142-44-42-140-40-14-12-34-92-64(108)26-22-60(86(131)132)100-62(88(135)136)24-32-72(117)118/h27-30,53-62,73-76,99-100H,7-26,31-52H2,1-6H3,(H,91,107)(H,92,108)(H,93,123)(H,94,124)(H,95,137)(H,96,138)(H,97,121)(H,98,122)(H,101,109)(H,102,110)(H,103,119)(H,104,120)(H,115,116)(H,117,118)(H,125,126)(H,127,128)(H,129,130)(H,131,132)(H,133,134)(H,135,136)/t55-,56-,57-,58-,59-,60+,61-,62-,73-,74-,75?,76?/m0/s1
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| InChIKey |
YCDAVYPOJRHJPE-GHMWWJSOSA-N
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| Pharmaceutical Properties |
Molecule Weight
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2088.198
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Polar area
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820.26
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Complexity
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.
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xlogp Value
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-4.2364
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Heavy Count
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146
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Rot Bonds
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85
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Hbond acc
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34
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Hbond Donor
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22
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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
wO2024239281A1 C207 [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) |
0.085 nM
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High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
C4-2B is both Steap1 and PSMA antigen high express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
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| In Vitro Model | Prostate carcinoma | C4-2B cells | CVCL_4784 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.11 nM
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High Steap1 and PSMA expression (Steapl and PSMA +++) | ||
| Method Description |
PC-3-4H7 cell is both Steap1and PSMA antigen high express cells. To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
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| In Vitro Model | Prostate carcinoma | PC-3-4H7 cells | Homo sapiens | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
10.9 nM
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Low Steap1 and PSMA expression (Steap1 and PSMA+) | ||
| Method Description |
22RV1 is both Steapl and PSMA antigen low express cells.To run the assay,the cells (180 ul,6000cells)were added to each well in a 96-well plate and incubated for 24 hours at 37°C with 5%CO 2. Next,the cells were treated with test compounds (20ul)at various concentrations in appropriate cell culture medium (total volume,0.2 mL).The control wells contain cells and the medium but lack the test compounds.The plates were incubated for 120 hours at 37°C with 5%CO 2.MTT (5 mg/mL)was then added to the wells (20ul)and the plates were incubated for 1.5 hr at 37°C.The medium was carefully removed and DMSO (180ul)was added afterward.After it was shaken for 15min, the absorbance was measured at 490 nm and 570 nm with a reference filter of 620 nm.The inhibition% was calculated according to the following equation:inhibition%=[1- (assay-blank)/ (control-blank)]× 100.
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| In Vitro Model | Prostate carcinoma | 22RV1 cells | CVCL_1045 | ||
References