Tezacitabine

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206004

CAS#: 130306-02-4

Description: Tezacitabine is a synthetic purine nucleoside analogue with potential antineoplastic activity. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication.


Chemical Structure

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Tezacitabine
CAS# 130306-02-4

Theoretical Analysis

MedKoo Cat#: 206004
Name: Tezacitabine
CAS#: 130306-02-4
Chemical Formula: C10H11FN2O4
Exact Mass: 242.07029
Molecular Weight: 242.2
Elemental Analysis: C, 49.59; H, 4.58; F, 7.84; N, 11.57; O, 26.42

Size Price Shipping out time Quantity
Inquire bulk and customized quantity

Pricing updated 2021-03-05. Prices are subject to change without notice.

Tezacitabine is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Synonym: MDL 101731; FMdC; KW 2331; MDL 101731; KW2331; MDL101731;

IUPAC/Chemical Name: 1-((2R,4S,5R,E)-3-(fluoromethylene)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one

InChi Key: CXVQYURZKMJITE-JZUREZDFSA-N

InChi Code: InChI=1S/C10H11FN2O4/c11-4-6-8(15)7(5-14)17-9(6)13-3-1-2-12-10(13)16/h1-4,7-9,14-15H,5H2/b6-4+/t7-,8+,9-/m1/s1

SMILES Code: O=C1N=CC=CN1[C@@H]2O[C@H](CO)[C@@H](O)/C2=C\F

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 242.2 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Taverna P, Rendahl K, Jekic-McMullen D, Shao Y, Aardalen K, Salangsang F, Doyle L, Moler E, Hibner B. Tezacitabine enhances the DNA-directed effects of fluoropyrimidines in human colon cancer cells and tumor xenografts. Biochem Pharmacol. 2007 Jan 1;73(1):44-55. Epub 2006 Sep 16. PubMed PMID: 17046720.

2: Skierski JS, Koronkiewicz M, Grieb P. Tezacitabine blocks tumor cells in G1 and S phases of the cell cycle and induces apoptotic cell death. Acta Pol Pharm. 2005 May-Jun;62(3):195-205. PubMed PMID: 16193812.

3: Stachnik K, Grieb P, Skierski JS. Cytotoxic effects of cladribine and tezacitabine toward HL-60. Acta Biochim Pol. 2005;52(2):561-5. Epub 2005 May 31. PubMed PMID: 15933759.

4: Bendell JC, Eder JP, Clark JW, Fidias P, Lynch TJ, Seiden MV, Ryan DP. Phase I dose-escalation study of tezacitabine in combination with 5-fluorouracil in patients with advanced solid tumors. Cancer. 2005 May 1;103(9):1925-31. PubMed PMID: 15772958.

5: Flaherty KT, Stevenson JP, Gallagher M, Giantonio B, Algazy KM, Sun W, Haller DG, O'Dwyer PJ. Dose escalation study of tezacitabine in combination with cisplatin in patients with advanced cancer. Cancer. 2003 Apr 15;97(8):1985-90. PubMed PMID: 12673728.

6: Rodriguez GI, Jones RE, Orenberg EK, Stoltz ML, Brooks DJ. Phase I clinical trials of tezacitabine [(E)-2'-deoxy-2'-(fluoromethylene)cytidine] in patients with refractory solid tumors. Clin Cancer Res. 2002 Sep;8(9):2828-34. PubMed PMID: 12231523.

7: Seley KL. Tezacitabine Hoechst Marion Roussel. Curr Opin Investig Drugs. 2000 Sep;1(1):135-40. Review. PubMed PMID: 11249589.



Additional Information