A CDK/CRK-specific kinase inhibitor
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CDK/CRK Inhibitor

Item No. 21195

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(2,6-dichlorophenyl)-1,5-dihydro-6-[[4-(2-hydroxyethoxy)phenyl]methyl]-3-(1-methylethyl)-4H-pyrazolo[3,4-d]pyrimidin-4-one
CAS Number
784211-09-2
Synonyms
  • Cdk7 Inhibitor IV
  • Cyclin-dependent kinase 7 Inhibitor IV
  • Cyclin-dependent kinase/CDK-related kinase Inhibitor
  • RGB-286147
Molecular Formula
C23H22Cl2N4O3
Formula Weight
473.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
214 nm
SMILES
O=C1C2=C(N(C3=C(Cl)C=CC=C3Cl)N=C2C(C)C)NC(CC4=CC=C(OCCO)C=C4)=N1
InChi Code
InChI=1S/C23H22Cl2N4O3/c1-13(2)20-19-22(29(28-20)21-16(24)4-3-5-17(21)25)26-18(27-23(19)31)12-14-6-8-15(9-7-14)32-11-10-30/h3-9,13,30H,10-12H2,1-2H3,(H,26,27,31)
InChi Key
RSQPNXBTPUXMQN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CDK/CRK inhibitor is an inhibitor of cyclin-dependent kinases (CDK) and CDK-related kinases (CRK) with IC50 values ranging from 9-839 nM in vitro.1 It is selective, exhibiting less than 20% inhibition of 60 non-CDK/CRK kinases, at a concentration of 1 μM. CDK/CRK inhibitor induces cell cycle arrest in the G1 phase, endoreduplication, and apoptosis in HCT116 cells. It exhibits broad anti-tumor activity with an average GI50 value of <10 nM for 60 tumorigenic cell lines. It also inhibits growth of non-cycling HCT116 cells with an IC50 value of 40 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Caligiuri, M., Becker, F.F., Murthi, K., et al. A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. Chem. Biol. 12(10), 1103-1115 (2005).