Linker Information
General Information of This Linker
| Linker ID |
LIN0PFNSS
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| Linker Name |
BGA7650 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 |
C10H19NO3S2
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| Isosmiles |
CC(CCC(O)=O)(SSCCCC(N)=O)C
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| InChI |
InChI=1S/C10H19NO3S2/c1-10(2,6-5-9(13)14)16-15-7-3-4-8(11)12/h3-7H2,1-2H3,(H2,11,12)(H,13,14)
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| InChIKey |
NLOYQTKSVQIMER-UHFFFAOYSA-N
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| Pharmaceutical Properties |
Molecule Weight
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265.4
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Polar area
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80.39
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Complexity
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220.1928095
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xlogp Value
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2.2767
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Heavy Count
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16
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Rot Bonds
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9
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Hbond acc
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4
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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
BGA7650 [Investigative]
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth lnhibition value (TGl) |
22%
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously
administered vehicle, BGA7650 (4 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly.
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| In Vivo Model | Human patient-derived gastric xenograft model | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.16 nM
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Lung adenocarcinoma | NCI-H2122 cells | CVCL_1531 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.55 nM
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Gastric adenocarcinoma | MKN45 cells | CVCL_0434 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
1.44 nM
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Positive CEA expression (CEA+++/++) | ||
| Method Description |
Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Colon adenocarcinoma | Ls147T cells | CVCL_1384 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
20 nM
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Negative CEA expression (CEA-) | ||
| Method Description |
MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||