2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis Nucleoside Antimetabolite/Analog
  4. Ethynylcytidine

Ethynylcytidine  (Synonyms: ECyD; TAS-106; 3'-C-Ethynylcytidine)

Cat. No.: HY-16200 Purity: 99.97%
COA Handling Instructions

Molarity Calculator

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. Ethynylcytidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

Ethynylcytidine Chemical Structure

Ethynylcytidine Chemical Structure

CAS No. : 180300-43-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
5 mg USD 140 In-stock
10 mg USD 240 In-stock
25 mg USD 540 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Ethynylcytidine Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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]. Ethynylcytidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

nucleoside antimetabolite[1]
In Vitro

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. These results suggest that the cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The differences in IC50 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 IC50 values at submicromolar concentrations in 4 of the 5 human tumors[1].

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

Ethynylcytidine Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

267.24

Formula

C11H13N3O5
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

OC[C@@H]1[C@](O)(C#C)[C@@H](O)[C@H](N2C(N=C(N)C=C2)=O)O1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (935.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.97%

COA (252 KB) HNMR (264 KB) RP-HPLC (243 KB) MS (68 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

MIAPaCa-2 cells are maintained in Dulbecco’s modified Eagle’s medium supplemented with 10% FCS and 2.5% horse serum. Cells in the exponential growth phase are seeded onto 6-well plates (5×104 cells/1.8 mL/well) on day 0. Twenty-four hours after seeding, on day 1, Ethynylcytidine (TAS-106) (6 concentrations range from 0 to 100 μM) is added to cultured cells (3 wells at each concentration) at a volume of 0.2 mL/well. After 4 and 24 h, on the 4 and 24 h Ethynylcytidine exposure schedules, the drug-containing medium is removed, and the cells are washed twice with Dulbecco’s phosphate buffered saline and subsequently cultured in drug-free medium until day 4. On the 72 h exposure schedule, after adding the Ethynylcytidine, cells are cultured continuously until day 4. On day 4, cell numbers are determined and converted to values related to the cell numbers on day 1. The concentration of Ethynylcytidine which inhibits cell growth by 50% (IC50) is calculated from this relative cell growth. Two or three individual experiments are conducted on each cell line to confirm reproducibility[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Nude rats s.c. transplanted with LX-1 human lung tumors are given a single i.v. dose of [3H]Ethynylcytidine (TAS-106) (6 mg/kg, 3.7 MBq/kg). For analysis of the distribution of radioactivity and intratumoral Ethynylcytidine metabolism, serum and various tissues (tumor, skin, lung, liver, kidney, spleen, small intestine, large intestine, testis, brain, and bone marrow cells) are sampled from 3 rats at each of the following 6 time points: 0.5, 1, 2, 4, 8 and 24 h after i.v. administration. At each point in time, bone marrow cells are collected from the 3 rats and combined into a cell pellet. All samples of serum, bone marrow cell pellets, and tissues are immediately frozen on dry ice and stored at -30°C until used[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7420 mL 18.7098 mL 37.4195 mL 93.5489 mL
5 mM 0.7484 mL 3.7420 mL 7.4839 mL 18.7098 mL
10 mM 0.3742 mL 1.8710 mL 3.7420 mL 9.3549 mL
15 mM 0.2495 mL 1.2473 mL 2.4946 mL 6.2366 mL
20 mM 0.1871 mL 0.9355 mL 1.8710 mL 4.6774 mL
25 mM 0.1497 mL 0.7484 mL 1.4968 mL 3.7420 mL
30 mM 0.1247 mL 0.6237 mL 1.2473 mL 3.1183 mL
40 mM 0.0935 mL 0.4677 mL 0.9355 mL 2.3387 mL
50 mM 0.0748 mL 0.3742 mL 0.7484 mL 1.8710 mL
60 mM 0.0624 mL 0.3118 mL 0.6237 mL 1.5591 mL
80 mM 0.0468 mL 0.2339 mL 0.4677 mL 1.1694 mL
100 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9355 mL
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Ethynylcytidine Related Classifications

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:

Ethynylcytidine180300-43-0ECyD TAS-106 3'-C-EthynylcytidineTAS106TAS 106TAS-106DNA/RNA SynthesisNucleoside Antimetabolite/AnalognucleosideanalogRNApolymerasesantitumorFM3AcellsInhibitorinhibitorinhibit

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