Linker Information
General Information of This Linker
| Linker ID |
LIN0UULHM
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| Linker Name |
Electron-deficient sulfonamide-based cleavable linker 10
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| Linker Type |
Reduction sensitive linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C31H42N6O11S
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| Isosmiles |
OCC1=CC=C(N(S(C2=NC=C(C#N)C=C2)(=O)=O)CCOCCOCCOCCN3C=C(N=N3)COCCOCCOCCC(O)=O)C=C1
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| InChI |
InChI=1S/C31H42N6O11S/c32-21-27-3-6-30(33-22-27)49(41,42)37(29-4-1-26(24-38)2-5-29)9-12-45-15-18-46-17-14-44-11-8-36-23-28(34-35-36)25-48-20-19-47-16-13-43-10-7-31(39)40/h1-6,22-23,38H,7-20,24-25H2,(H,39,40)
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| InChIKey |
GIBBPMVMOZYLBK-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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706.775
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Polar area
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217.68
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Complexity
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1447.980472
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xlogp Value
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1.00688
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Heavy Count
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49
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Rot Bonds
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27
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Hbond acc
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15
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Hbond Donor
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2
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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
39424599 ADC-10A [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) |
0.98 nM
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Positive FR expression (FR+++/++) | ||
| Method Description |
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.
Click to Show/Hide
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| In Vitro Model | Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma | IGROV1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
37.235 nM
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Negative FR expression (FR-) | ||
| Method Description |
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.
Click to Show/Hide
|
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| In Vitro Model | Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma | IGROV1 cells | CVCL_1304 | ||
39424599 ADC-10B [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) |
24.505 nM
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Positive FR expression (FR+++/++) | ||
| Method Description |
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.
Click to Show/Hide
|
||||
| In Vitro Model | Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma | IGROV1 cells | CVCL_1304 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
36.665 nM
|
Negative FR expression (FR-) | ||
| Method Description |
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.
Click to Show/Hide
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| In Vitro Model | Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma | IGROV1 cells | CVCL_1304 | ||
References