CDK9-IN-12

SKU: orb1691377

Description

CDK9-IN-12 is a potent and selective CDK9 inhibitor used in leukemia research. It suppresses oncogenic transcription, leading to proliferation arrest and apoptosis in cancer cells, as demonstrated in various in vitro and in vivo preclinical studies.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1942843-54-0
• MW: 378.86
• Purity: 98.93% (May vary between batches)
• Formula: C₂₁H₁₉ClN₄O
• SMILES: ClC1=C(C=2C=C3C(=CC2)NN=C3C)C=C(N[C@@H](CO)C4=CC=CC=C4)C=N1
• Target: CDK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.71 mM);DMSO:80 mg/mL (211.16 mM)

Bioactivity

• Target IC50:
  CDK9-CyclinT1:5.41 nM
• In Vivo:
  Methods: CDK9-IN-12 (7.5 mg/kg, 0.5% CMC-Na, gavage, 21 days) was used to treat MV-4-11 cell tumor xenograft model mice. First, PK experiments were performed in mice. Second, the diameter of the transplanted tumor and the weight of the mice were measured twice a week to evaluate the in vivo anticancer effect. Results: CDK9-IN-12 has a long half-life (t1/2 = 8.02 h) and acceptable bioavailability (F = 33.7%). In addition, CDK9-IN-12 can significantly inhibit tumor progression, with a T/C value of 27.80%.
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• In Vitro:
  CDK9-IN-12 has an inhibitory effect on the following cells: Mino, Z-138, JeKo-1, Raji, OCI-Ly-10, TMD8, MM.1S, RPMI-8226, Kasumi-1, HL-60, CCRF-CEM, MV-4-11 cells with IC50 values ​​of 8.4, 46, 46, 37, 3.2, 46, 1.5, 5.4, 21, 44, 2.1, 1.6 nM, respectively.
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Storage & Handling

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

Alternative Names

CDK9IN12, CDK-9-IN-12, CDK9-IN-12, CDK9 IN 12

Compound Identifiers

PubChem CID

162640599