An antiproliferative cyclin D1/Cdk4 inhibitor
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Cdk4 Inhibitor

Item No. 17648

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione
CAS Number
546102-60-7
Synonyms
  • Cyclin-dependent kinase 4 Inhibitor
Molecular Formula
C20H10BrN3O2
Formula Weight
404.2
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 0.25 mg/ml
λmax
236, 259, 271, 283, 318, 397 nm
SMILES
O=C1NC(C2=C1C(C(C=CC(Br)=C3)=C3N4)=C4C5=C2C6=C(C=CC=C6)N5)=O
InChi Code
InChI=1S/C20H10BrN3O2/c21-8-5-6-10-12(7-8)23-18-14(10)16-15(19(25)24-20(16)26)13-9-3-1-2-4-11(9)22-17(13)18/h1-7,22-23H,(H,24,25,26)
InChi Key
NMFKDDRQSNVETB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $75

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    1 mg

    $128

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    5 mg

    $553

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    Product Description

    Cdk4 inhibitor is a cell-permeable, asymmetrical indolocarbazole that exhibits antiproliferative activity by blocking cyclin D1/Cdk4 with an IC50 value of 0.8 μM.1 It is selective for cyclin D1/Cdk4, demonstrating 7-fold and 28-fold weaker activity against cyclin E/Cdk2 and cyclin B/Cdk1, respectively, and little activity against calcium/calmodulin-dependent protein kinase II and protein kinase A.1 This compound has been shown to inhibit HCT116 and NCI-H460 tumor cell growth (IC50s < 3.0 μM) by blocking retinoblastoma protein phosphorylation and inducing G1 cell cycle arrest.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhu, G., Conner, S.E., Zhou, X., et al. Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J. Med. Chem. 46(11), 2027-2030 (2003).