CAN508

SKU: orb1298625

Description

CAN508 is a potent and selective ATP-competitive inhibitor of CDK9/cyclin T1 (IC50=0.35 μM), showing 38-fold selectivity over other CDKs like CDK2/cyclin E. Its mechanism supports its investigation as a potential antitumor agent in cancer research, applicable for both in vitro biochemical assays and cellular studies.

Research Area

Cell Biology

Key Properties

• CAS Number: 140651-18-9
• MW: 218.22
• Purity: 98.65% (May vary between batches)
• Formula: C₉H₁₀N₆O
• SMILES: Nc1n[nH]c(N)c1\N=N\c1ccc(O)cc1
• Target: CDK
• Solubility: DMSO:250 mg/mL (1145.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (22.91 mM)

Bioactivity

• Target IC50:
  CDK9-CyclinT1:0.35 μM|CDK2-CyclinE:20 μM|CDK1-CyclinB:44 μM|CDK7-CyclinH:26 μM|Cdk4-CyclinD1:13.5 μM|CDK2-CyclinA:69 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ATP-competitive, CAN 508, CAN508, CAN-508, adenocarcinoma, Cyclin dependent kinase, cells, CDK9/cyclin T1, CDK, inhibit, Inhibitor, HT-29, esophageal

Compound Identifiers

PubChem CID

135398514