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Ethynylcytidine

Catalog No. TQ0006 CAS 180300-43-0

Synonyms: TAS-106, 3'-C-Ethynylcytidine, ECyD

Ethynylcytidine is a nucleoside antimetabolite.

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Ethynylcytidine, CAS 180300-43-0

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ethynylcytidine is a nucleoside antimetabolite.
In vitro	The cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The IC50 values of Ethynylcytidine in the five human tumors with 4, 24 and 72 h exposure range from 0.114 to 1.032 μM, 0.015 to 0.067 μM, and 0.008 to 0.058 μM, respectively. The differences in IC50 values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appears to show sufficiently potent cytotoxicity at the 24 h exposure time in all 5 human tumors.
In vivo	In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with a tumor growth inhibition rate on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine on all three administration schedules. In particular, the administration of Ethynylcytidine at 6 mg/kg once weekly exhibits a marked tumor-shrinking effect with an IR of 98% against the LX-1 tumor. While Ethynylcytidine treatment on an either 3 or 5 times weekly schedule has a potent antitumor effect with an IR of approximately 85%, the IR of Ethynylcytidine once weekly is less than 60% and its antitumor effect is rather weak.

Synonyms	TAS-106, 3'-C-Ethynylcytidine, ECyD
Molecular Weight	267.24
Formula	C11H13N3O5
CAS No.	180300-43-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 240 mg/mL (898.07 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Shimamoto Y, et al. Antitumor activity and pharmacokinetics of TAS-106, 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine. Jpn J Cancer Res. 2001 Mar;92(3):343-51.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ethynylcytidine 180300-43-0 DNA损伤和修复细胞周期 Nucleoside Antimetabolite/Analog 3'-C-Ethynylcytidine ECyD TAS-106 Inhibitor inhibitor inhibit

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