Cdk4/6 Inhibitor IV

Catalog No. Size PriceQuantity
M22120-C Contact for quotation $100Unavailable


Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine inhibitor for Cdk4/cyclin D1 and Cdk6/cyclin D1 . Cyclin-dependent kinase 4 (Cdk4) is an important cell cycle kinase, since its activity is required for initiating the phosphorylation of the retinoblastoma protein (pRb). Hyperphosphorylation of pRb prevents cells from initiating DNA synthesis, releases the sequestered transcription factors, leading to the loss of pRb's growth-inhibitory function, thus allowing cells to enter S phase . In vitro: Cdk4/6 inhibitor IV showed an inhibitory effect on Cdk4/cyclin D1 and Cdk6/cyclin D1with the IC50 values of 1.5 and 5.6 μM, respectively. Cdk4/6 inhibitor IV exihibited potent selectivity for Cdk4/6 over Cdk5/p35, c-met, v-abl, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B with the IC50 values ≥ 10-100 μM. In asynchronous cell lines, at 5-10 μM, Cdk4/6 inhibitor IV blocked retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis. In vivo: In mice xenografted with human HCT116 colon carcinoma, treatment with of Cdk4/6 inhibitor IV (i.p, 30 mg/kg) after 29 days suppressed tumor growth.

Product information

CAS Number: 359886-84-3

Molecular Weight: 456.58

Formula: C27H32N6O

Chemical Name: (1r,4r)-4-({2-[(1-benzyl-1H-indol-5-yl)amino]-6-(ethylamino)pyrimidin-4-yl}amino)cyclohexan-1-ol

Smiles: CCNC1C=C(N[C@@H]2CC[C@@H](O)CC2)N=C(NC2=CC=C3C(C=CN3CC3=CC=CC=C3)=C2)N=1


InChi: InChI=1S/C27H32N6O/c1-2-28-25-17-26(29-21-8-11-23(34)12-9-21)32-27(31-25)30-22-10-13-24-20(16-22)14-15-33(24)18-19-6-4-3-5-7-19/h3-7,10,13-17,21,23,34H,2,8-9,11-12,18H2,1H3,(H3,28,29,30,31,32)/t21-,23-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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