Thiarabine hydrochloride
Thiarabine (OSI-7836) hydrochloride is an orally active cytotoxic antitumor agent that acts as a deoxycytidine kinase substrate and a DNA chain terminator. Thiarabine hydrochloride is metabolized to form its major active metabolite T-araCTP, which potently inhibits DNA synthesis and exhibits a long retention time in tumor cells. Thiarabine hydrochloride is widely applicable to research related to leukemia, lymphoma, hematologic malignancies, acute myeloid leukemia, and advanced solid malignancies.
For research use only. We do not sell to patients.
- CAS No.: 1060763-87-2
- Formula: C9H14ClN3O4S
- Molecular Weight:295.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Thiarabine hydrochloride (1-10 μM) potently inhibits the growth of a panel of human tumor cell lines with IC50 values of 1 to 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Thiarabine (22.5-90 mg/kg/dose; i.p.; daily; 9 consecutive days, days 1-9) hydrochloride is fully ineffective against thiarabine-resistant P388/T-araC leukemia in CD2F1 mice[1].
Thiarabine (100 mg/kg/dose; i.p.; single dose) hydrochloride is converted to its active metabolite T-araCTP at comparable levels in both thiarabine-sensitive P388/0 and thiarabine-resistant P388/T-araC leukemia cells in CD2F1 mice following a 100 mg/kg i.p. dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD2F1 Mice (female, implanted intraperitoneally with 10^6 parental P388/0 leukemia cells)[1]
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Dosage:45 mg/kg/dose; 90 mg/kg/dose
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Administration:i.p.; daily; 9 consecutive days (days 1-9)
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Result:Produced a median increase in lifespan (ILS) of +136% in passage 0 parental P388/0-bearing mice, with a median treated lifespan of 26.0 days versus 11.0 days in untreated controls.
Produced median ILS values ranging from +163% to +220% and net log10 cell kill values ranging from +6.3 to >6.9 units (approximately 1,000,000-fold reduction in tumor burden) across four studies in parental P388/0-bearing mice; 1/6 mice were long-term (60-day) survivors in two of these studies.
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Animal Model:CD2F1 Mice (female, implanted intraperitoneally with 10^6 thiarabine-resistant P388/T-araC leukemia cells)[1]
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Dosage:22.5 mg/kg/dose; 45 mg/kg/dose; 90 mg/kg/dose
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Administration:i.p.; daily; 9 consecutive days (days 1-9)
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Result:Produced median ILS values ranging from +4% to +13% across passage 8, 21, and selection studies in P388/T-araC-bearing mice, with median treated lifespans only marginally longer than untreated controls.
Produced median ILS values ranging from 0% to +9% and net log10 cell kill values of -1.8 to -1.9 units (almost 100-fold leukemia growth during treatment) across four studies in P388/T-araC-bearing mice; no long-term (60-day) survivors were observed.
Produced a median ILS of +8% in passage 8 P388/T-araC-bearing mice.
Chemical Information
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CAS No. 1060763-87-2
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Molecular Weight 295.74
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Formula C9H14ClN3O4S
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SMILES
O[C@@H]1[C@H](N2C(N=C(C=C2)N)=O)S[C@@H]([C@H]1O)CO.Cl
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Synonyms
OSI-7836 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Waud WR, et al.. Isolation and characterization of a murine P388 leukemia line resistant to thiarabine. Nucleosides, nucleotides & nucleic acids. 2012;31(1):14-27. [Content Brief]
[2]. Parker WB, et al.. Thiarabine, 1-(4-Thio-β-D-arabinofuranosyl)cytosine. A Deoxycytidine Analog With Excellent Anticancer Activity. Current medicinal chemistry. 2015;22(34):3881-96. [Content Brief]
[3]. Jordheim LP, et al.. Advances in the development of nucleoside and nucleotide analogues for cancer and viral diseases. Nature reviews. Drug discovery. 2013 Jun;12(6):447-64. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Thiarabine hydrochloride Related Classifications
HY-16496A Related Classifications
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