OBI-3424 (TH-3424) | DNA alkylating agent

Chemical Structure : OBI-3424

CAS No.: 2097713-68-1

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

Catalog No.: PC-35531Not For Human Use, Lab Use Only.

OBI-3424 (AST-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.

Packing	Price	Stock
5 mg	$218	In stock
10 mg	$358	In stock
25 mg	$548	In stock
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Biological Activity

OBI-3424 (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.

Physicochemical Properties

M.Wt	460.427
Formula	C21H25N4O6P
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-1-(3-(3-(dimethylcarbamoyl)phenoxy)-4-nitrophenyl)ethyl di(aziridin-1-yl)phosphinate

References

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.

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

Biological Activity

Physicochemical Properties

References

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