1. Cell Cycle/DNA Damage
  2. CDK
  3. CAN508

CAN508 

Cat. No.: HY-100429
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CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.

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

CAN508 Chemical Structure

CAN508 Chemical Structure

CAS No. : 140651-18-9

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Description

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity[1][2].

IC50 & Target[1]

CDK9/cyclinT1

0.35 μM (IC50)

CDK2/cyclinE

20 μM (IC50)

cdk2/cyclin A

69 μM (IC50)

Cdk4/cyclin D1

13.5 μM (IC50)

CDK7/cyclin H

26 μM (IC50)

Cdk1/cyclin B

44 μM (IC50)

In Vitro

CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays[1].
CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM[2].
CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells[2].

Apoptosis Analysis[1]

Cell Line: SKGT4, OE33 and FLO-1 cells
Concentration: 40 μM
Incubation Time: 72 hours
Result: Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.
In Vivo

CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[1].

Animal Model: 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1]
Dosage: 60 mg/kg
Administration: I.p.; daily for 10 days
Result: Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.
Molecular Weight

218.22

Formula

C₉H₁₀N₆O

CAS No.

140651-18-9

SMILES

OC1=CC=C(/N=N/C2=C(N)NN=C2N)C=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CAN508CAN 508CAN-508CDKCyclin dependent kinaseHT-29cellsesophagealadenocarcinomaATP-competitiveInhibitorinhibitorinhibit

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