[CAS NO. 180300-43-0] Ethynylcytidine

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PRODUCTS SPECIFICATIONS [180300-43-0]

Catalog

HY-16200

Brand

MCE

CAS

180300-43-0

DESCRIPTION [180300-43-0]

Overview

MDL	-
Molecular Weight	267.24
Molecular Formula	C11H13N3O5
SMILES	OC[C@@H]1[C@@]([C@H]([C@H](N2C(N=C(C=C2)N)=O)O1)O)(C#C)O

For research use only. We do not sell to patients.

Summary

Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis , inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer ^[1] ^[2] ^[3] .

IC50 & Target

nucleoside antimetabolite ^[1]

In Vitro

The IC ₅₀ 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. These results suggest that the cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The differences in IC ₅₀ values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appeares to show sufficiently potent cytotoxicity at the 24 h exposure time in all 5 human tumors. Even at the 4 h exposure time, Ethynylcytidine clearly shows potent cytotoxicity with IC ₅₀ values at submicromolar concentrations in 4 of the 5 human tumors ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with an tumor growth inhibition rate (IR) on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine (TAS-106) on all three administration schedules. In particular, 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 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00737360	Taiho Pharmaceutical Co., Ltd.	Head and Neck Cancer	August 2008	Phase 2
NCT00752011	M.D. Anderson Cancer Center\|Taiho Pharmaceutical Co., Ltd.	Cancer\|Solid Tumors	June 2008	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 935.49 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7420 mL	18.7098 mL	37.4195 mL
5 mM	0.7484 mL	3.7420 mL	7.4839 mL
10 mM	0.3742 mL	1.8710 mL	3.7420 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (7.78 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (7.78 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (7.78 mM); Clear solution

* All of the co-solvents are available by MCE.