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CAN508

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Catalog No. T8796Cas No. 140651-18-9

CAN508 is a potent ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Antitumor activity.]

CAN508

CAN508

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Purity: 98.65%
Catalog No. T8796Cas No. 140651-18-9
CAN508 is a potent ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Antitumor activity.]
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$30In StockIn Stock
10 mg$41In StockIn Stock
25 mg$88In StockIn Stock
50 mg$133In StockIn Stock
100 mg$198In StockIn Stock
200 mg$291-In Stock
1 mL x 10 mM (in DMSO)$34In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.65%
Appearance:Solid
Color:Black
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Product Introduction

Bioactivity
Description
CAN508 is a potent ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Antitumor activity.]
Targets&IC50
CDK9-CyclinT1:0.35 μM, CDK2-CyclinE:20 μM, CDK2-CyclinA:69 μM, CDK1-CyclinB:44 μM, Cdk4-CyclinD1:13.5 μM, CDK7-CyclinH:26 μM
In vitro
The most potent inhibitor,CAN508, reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.?Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9.
Chemical Properties
Molecular Weight218.22
FormulaC9H10N6O
Cas No.140651-18-9
SmilesNc1n[nH]c(N)c1\N=N\c1ccc(O)cc1
Relative Density.1.67 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (1145.63 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (22.91 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.5825 mL22.9127 mL45.8253 mL229.1266 mL
5 mM0.9165 mL4.5825 mL9.1651 mL45.8253 mL
10 mM0.4583 mL2.2913 mL4.5825 mL22.9127 mL
20 mM0.2291 mL1.1456 mL2.2913 mL11.4563 mL
50 mM0.0917 mL0.4583 mL0.9165 mL4.5825 mL
100 mM0.0458 mL0.2291 mL0.4583 mL2.2913 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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

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