| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
Purity: ≥98%
| ln Vivo |
Thiarabine is effective orally (bioavailability approximately 16%) and administered once daily; although thiorabine's structure and basic mechanism of action are similar to those of cytarabine, there are many quantitative differences in the biochemical pharmacology of these two drugs that may explain thiorabine's superior antitumor activity. Thiarabine also outperforms gemcitabine, clofarabine, and cytarabine in mice when it comes to antitumor activity. In contrast, thorabin showed excellent activity against solid tumor xenografts, indicating that the drug has potent activity in animal models that could lead to clinical applications.
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| References | |
| Additional Infomation |
OSI-7836 belongs to the nucleoside analogue of cytotoxic drugs, with gemcitabine being the market leader in this class. OSI Pharmaceuticals is developing OSI-7836 as a next-generation gemcitabine. The antitumor activity of OSI-7836 appears to be less affected by dosing regimens than gemcitabine. Its activity was higher than cytarabine (another clinically used nucleoside analogue) in all nine models tested; it was also higher than paclitaxel or cisplatin in the two lung xenograft models tested. No unexpected toxicities were observed; the observed toxicities were similar to those of other nucleoside analogues. Thiabine is an analogue of the antimetabolite cytarabine (ara-C) with potential antitumor activity. After administration, thiabine (T-araC) is phosphorylated to the triphosphate form T-araCTP, which competes with cytidine for incorporation into DNA. This leads to inhibition of DNA replication and RNA synthesis, chain termination, and may ultimately reduce tumor cell proliferation. Compared to cytarabine (ara-C), T-araC has a longer half-life and higher efficacy.
Drug indications Its use has been investigated in the treatment of solid tumors.Mechanism of action The mechanism by which OSI-7836 inhibits tumor growth appears to differ from gemcitabine; it blocks cell division at different stages of the cell cycle (G2 phase). Its mechanism of action involves phosphorylation to a triphosphate form, which is then incorporated into cellular DNA, ultimately leading to cell death. |
| Exact Mass |
259.062
|
|---|---|
| CAS # |
26599-17-7
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| PubChem CID |
168566
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| Appearance |
White to off-white solid powder
|
| Density |
1.9±0.1 g/cm3
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| Boiling Point |
535.0±60.0 °C at 760 mmHg
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| Flash Point |
277.4±32.9 °C
|
| Vapour Pressure |
0.0±3.2 mmHg at 25°C
|
| Index of Refraction |
1.814
|
| LogP |
-1.91
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
17
|
| Complexity |
386
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](S2)CO)O)O
|
| InChi Key |
GAKJJSAXUFZQTL-CCXZUQQUSA-N
|
| InChi Code |
InChI=1S/C9H13N3O4S/c10-5-1-2-12(9(16)11-5)8-7(15)6(14)4(3-13)17-8/h1-2,4,6-8,13-15H,3H2,(H2,10,11,16)/t4-,6-,7+,8-/m1/s1
|
| Chemical Name |
2(1H)-Pyrimidinone, 4-amino-1-(4-thio-beta-D-arabinofuranosyl)-
|
| Synonyms |
OSI-7836OSI 7836OSI7836
Thiarabine
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01139151 | COMPLETED | Drug: 3 Day Thiarabine Drug: 5 Day Thiarabine |
Leukemia | M.D. Anderson Cancer Center | 2010-08 | Phase 1 |
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