1. Cell Cycle/DNA Damage
  2. DNA Alkylator/Crosslinker
  3. OBI-3424

OBI-3424 (Synonyms: TH-3424)

Cat. No.: HY-124573
Handling Instructions

OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.

For research use only. We do not sell to patients.

OBI-3424 Chemical Structure

OBI-3424 Chemical Structure

CAS No. : 2097713-68-1

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Description

OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research[1].

In Vitro

OBI-3424 exerts potent cytotoxicity against the H460 lung cancer cell line (IC50 of 4.0 nM). OBI-3424 exhibits potent cytotoxicity, in particular against cell lines derived from T-ALL with high AKR1C3 expression, with IC50 values in the low nM range[1].
OBI-3424 also exerts potent cell killing against ALL PDXs, and the median IC50 values were 60.3 nM for B-ALL, 9.7 nM for T-ALL and 31.5 nM for ETP-ALL[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

OBI-3424 (0.5-2.5 mg/kg; i.p.; once weekly; for 3 weeks) treatment induces regressions in PDXs mice and results in prolongation of mouse event-free survival[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NSG mice (20-25 g) bearing patient-derived xenografts (PDX)[1]
Dosage: 0.5 mg/kg, 1 mg/kg, 2.5 mg/kg
Administration: Intraperitoneal injection; once weekly; for 3 weeks
Result: Resulted in prolongation of mouse event-free survival.
Molecular Weight

460.42

Formula

C₂₁H₂₅N₄O₆P

CAS No.
SMILES

O=P(N1CC1)(N2CC2)O[[email protected]@H](C3=CC=C([N+]([O-])=O)C(OC4=CC=CC(C(N(C)C)=O)=C4)=C3)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

OBI-3424TH-3424OBI3424OBI 3424TH3424TH 3424DNA Alkylator/CrosslinkerAKR1C3DNA-alkylatingALLanticancerInhibitorinhibitorinhibit

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OBI-3424
Cat. No.:
HY-124573
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