Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0QSGZZ
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| ADC Name |
wO2024239281A1 C207
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| Synonyms |
WO2024239281A1 C207
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| Organization |
HANGZHOU DAC BIOTECH CO., LTD
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
4.4
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| Structure |
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| Antibody Name |
Vandortuzumab
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Antibody Info | ||||
| Antigen Name |
Metalloreductase STEAP1 (STEAP1)
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Antigen Info | ||||
| Payload Name |
Exatecan-aminoethoxy
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase I (TOP1)
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Target Info | ||||
| Linker Name |
WO2024239281A1, C207, Linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
(3S,7S,32S,49S,74S,78S)-32,49-bis ((S)-1- ((S)-1- ((2- ((S)-4,11- diethyl-8-fluoro-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl)oxy)ethyl)amino)-1-oxopropan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)carbamoyl)-40,41-bis (2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5,10,26,34,39,42,47,55,71,76-decaoxo-14,17,20, 23,58,61,64,67-octaoxa-4,6,11,27,33,38,43,48,54,70,75,77-dodecaazaoctacontane-1,3,7,74,78,80-hexacarboxylic acid
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General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
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 | 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 | 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 | 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