Cdk4/6 Inhibitor IV

Names

[ Name ]:
Cdk4/6 Inhibitor IV

[Synonym ]:
CINK4
trans-4-({2-[(1-Benzyl-1H-indol-5-yl)amino]-6-(ethylamino)-4-pyrimidinyl}amino)cyclohexanol
Cyclohexanol, 4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-, trans-
trans-4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-cyclohexanol
CGP 82996
CGP-82996

Biological Activity

[Description]:

[In Vitro]

Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC50 = 1.5 ��M and 5.6 ��M for Cdk4/D1 and Cdk6/D1, respectively) with selectivity over Cdk5/p35 (IC50 = 25 ��M), v-abl, c-met, IGF-1R and IR (IC50 > 10 ��M), Cdk2/A, Cdk2/E, Cdk4/D2, Cdk6/D2 (IC50 > 50 ��M) and Cdk1/B (IC50 > 100 ��M). Cdk4/6 Inhibitor IV exhibits blocking of pRb phosphorylation at Ser780 and Ser795, induce cell cycle arrest (G0/G1), and apoptosis in U2OS and MRC-5 cells at 5 - 10 ��M. Further, suppresses tumor growth in Xenograft mouse model (30 mg/kg, i.p.).

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
755.4±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₇H₃₂N₆O

[ Molecular Weight ]:
456.583

[ Flash Point ]:
410.6±35.7 °C

[ Exact Mass ]:
456.263763

[ LogP ]:
4.01

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.680

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310 + P330

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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