2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. Thiarabine hydrochloride

Thiarabine hydrochloride  (Synonyms: OSI-7836 hydrochloride)

Cat. No.: HY-16496A
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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.

Thiarabine hydrochloride

Thiarabine hydrochloride Chemical Structure

CAS No. : 1060763-87-2

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Description

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[1][2][3].

In Vitro

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 hydrochloride Related Antibodies
In Vivo

Thiarabine (45-90 mg/kg/dose; i.p.; daily; 9 consecutive days, days 1-9) exhibits potent in vivo antitumor activity against parental P388/0 leukemia in CD2F1 mice[1].
Thiarabine (22.5-90 mg/kg/dose; i.p.; daily; 9 consecutive days, days 1-9) is fully ineffective against thiarabine-resistant P388/T-araC leukemia in CD2F1 mice[1].
Thiarabine (100 mg/kg/dose; i.p.; single dose) 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.

Animal Model: CD2F1 Mice (female, implanted intraperitoneally with 10^6 parental P388/0 leukemia cells)[1]
Dosage: 45 mg/kg/dose; 90 mg/kg/dose
Administration: i.p.; daily; 9 consecutive days (days 1-9)
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.
Animal Model: CD2F1 Mice (female, implanted intraperitoneally with 10^6 thiarabine-resistant P388/T-araC leukemia cells)[1]
Dosage: 22.5 mg/kg/dose; 45 mg/kg/dose; 90 mg/kg/dose
Administration: i.p.; daily; 9 consecutive days (days 1-9)
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.
Molecular Weight

295.74

Formula

C9H14ClN3O4S
CAS No.
SMILES

O[C@@H]1[C@H](N2C(N=C(C=C2)N)=O)S[C@@H]([C@H]1O)CO.Cl
Shipping

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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References
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Thiarabine hydrochloride Related Classifications

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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.

Keywords:

Thiarabine1060763-87-2OSI-7836OSI7836OSI 7836DNA/RNA Synthesislymphoma xenograftsDNA chain terminatorDNA synthesisdeoxycytidine kinaseP388/0 leukemia cellsacute myelogenous leukemialeukemia xenograftshematologic malignanciesleukemia cellshuman solid tumorInhibitorinhibitorinhibit

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