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AST-3424 (S-isomer)

Chemical Structure : AST-3424 (S-isomer)

CAS No.: 2097713-69-2

AST-3424 (S-isomer) (OBI-3424 (S-isomer), TH-3424 (S-isomer))

货号: 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.

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10 mg ¥2980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 460.427
分子式 C21H25N4O6P
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-(3-(3-(dimethylcarbamoyl)phenoxy)-4-nitrophenyl)ethyl di(aziridin-1-yl)phosphinate

参考文献

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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