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  3. Odafosfamide

Odafosfamide  (Synonyms: (S)-OBI-3424; (S)-TH-3424; AST-3424)

Cat. No.: HY-149040
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Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research.

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

Odafosfamide

Odafosfamide Chemical Structure

CAS No. : 2097713-69-2

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Description

Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research[1][2].

In Vitro

Odafosfamide (72-96 h) shows cytotoxicity against liver cancer cells (SNU-475, SNU-449, C3A, with IC50s of 15 nM, 45 nM, 5 nM, respectively) and non-small cell lung cancer cells (NSCLC) (NCI-H1944, NCI-H2228, NCIH1755, NCI-H1563, NCI-H2110, NCI-H1792, with IC50s of 2.3 nM, 0.21 nM, 8.2 nM, 2.5 nM, 1.1 nM, 4.5 nM, respectively) with high AKR1C3 protein and RNA expression levels[1].

Odafosfamide shows potent anti-leukemic activity against 19 leukemia cell lines representing B-ALL, T-ALL, and ETP-ALL (IC50s values were 60.3 nmol/L, 9.7 nmol/L, and 31.5 nmol/L, respectively)[2].

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

In Vivo

Odafosfamide (1.25-5 mg/kg, i.v., once a week, 2 weeks) inhibits tumor growth in HepG2 orthotopic xenograft mice model[1].

Odafosfamide (0.625-1.25 mg/kg, i.v., weekly for 2 cycles; with one week off, and another 2 cycles of weekly) inhibits tumor growth in H460 subcutaneous mice model[1].

Odafosfamide (2.5 mg/kg, 5 mg/kg, i.v., weekly for 4-5 doses) inhibits tumor growth in (CRPC) VCaP, SNU-16 and A498 xenograft mice model[1].

Odafosfamide (1.25-5 mg/kg, i.v., once a week, 3 weeks) inhibits tumor growth in PA1280, GA6201 and LU2505 xenograft mice model[1].

Odafosfamide (2.5 mg/kg, i.p., once weekly × 3 weeks) induces substantial and prolonged regressions of disease in PDX mice models of pediatric ALL[2].

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

Animal Model: HepG2 orthotopic xenograft (~1 mm3 in diameter) female athymic nude mice (6 weeks; BALB/c-nu) model[1]
Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg
Administration: i.v., once a week, 2 weeks
Result: Inhibited tumor growth, with growth inhibition (TGI) at Day 34 of 52.4% at 1.25 mg/kg, 91.5% at 2.5 mg/kg and 101.2% at 5 mg/kg, respectively.
Animal Model: (CRPC) VCaP xenograft male BALB/c nude mice model[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: i.v., weekly for 5 doses
Result: Inhibited tumor growth, with growth inhibition of 148% at 5 mg/kg, further enhanced to 158% when combined with Abiraterone (HY-70013)/Prednisolone (HY-17463).
Animal Model: PDX (female 20–25 g) NSG mice models of pediatric ALL[2]
Dosage: 2.5 mg/kg
Administration: i.p., once weekly × 3 weeks
Result: Induced substantial and prolonged regressions of disease in All-8, ALL-27, ALL-29, ALL-30, ALL-31, ALL-28,ALL-AKR1C3, combined with Nelarabine (HY-13701) resulted in prolongation of mouse EFS compared with each single agent alone.
Molecular Weight

460.42

Formula

C21H25N4O6P

CAS No.
SMILES

C[C@@H](C1=CC(OC2=CC(C(N(C)C)=O)=CC=C2)=C(C=C1)[N+]([O-])=O)OP(N3CC3)(N4CC4)=O

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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.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Odafosfamide
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