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Chemical Structure : AST-3424 (S-isomer)
CAS No.: 2097713-69-2
Catalog No.: PC-38759Not For Human Use, Lab Use Only.
OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $488 | In stock | |
| 100 mg | Get quote | ||
| 1 g | Get quote |
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OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.
OBI-3424 exerted potent cytotoxicity against the H460 lung cancer cell line (IC50 4.0 nM), and potent cytotoxicity, in particular against cell lines derived from T-ALL with high AKR1C3 expression, with IC50 values in the low nM range.
OBI-3424 shows potential anti-leukemic activity against a panel of 19 PDXs representative of B-ALL, T-ALL and ETP-ALL (median IC50=60.3 nM).
OBI-3424 exerted profound in vivo efficacy against T-ALL PDXs, OBI-3424 combined with nelarabine resulted in prolongation of mouse EFS compared with each single agent alone.
| M.Wt | 460.427 | |
| Formula | C21H25N4O6P | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-1-(3-(3-(dimethylcarbamoyl)phenoxy)-4-nitrophenyl)ethyl di(aziridin-1-yl)phosphinate |
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1. Richard B. Lock, et al. Abstract LB-B16: The AKR1C3-Activated Prodrug OBI-3424 Exerts Profound In Vivo Efficacy Against Preclinical Models of T-Cell Acute Lymphoblastic Leukemia (T-ALL); a Pediatric Preclinical Testing Consortium Study. AACR 2018.
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