Cdk4/6 Inhibitor IVA cell-permeable triaminopyrimidine compound and inhibitor of Cdk4/6

Cdk4/6 Inhibitor IV (CAS 359886-84-3)

Cdk4/6 Inhibitor IV | CAS 359886-84-3 is rated 5.0 out of 5 by 1.
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Synonym: CINK4
Application: A cell-permeable triaminopyrimidine compound and inhibitor of Cdk4/6
CAS Number: 359886-84-3
Purity: >95%
Molecular Weight: 456.6
Molecular Formula: C27H32N6O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC50 = 1.5 µM and 5.6 µM for Cdk4/D1 and Cdk6/D1, respectively) with selectivity over Cdk5/p35 (IC50 = 25 µM), v-abl, c-met, IGF-1R and IR (IC50 > 10 µM), Cdk2/A, Cdk2/E, Cdk4/D2, Cdk6/D2 (IC50 > 50 µM) and Cdk1/B (IC50 > 100 µM). 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 µM. Further, suppresses tumor growth in Xenograft mouse model (30 mg/kg, i.p.).


References

Soni, R., et al. 2001. J. Natl. Cancer Inst. 93, 436.

Physical State :
Solid
Solubility :
Soluble in DMSO.
Storage :
Store at -20° C
IC50 :
Cdk4 : IC50 = 1.5 µM; Cdk6: IC50 = 5.6 µM; Cdk5/p35: IC50 = 25 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

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Cdk4/6 Inhibitor IV  Product Citations

See how others have used Cdk4/6 Inhibitor IV. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 26851223  2016. J. Immunol. 196: 2870-8.

PMID: # 27192561  2016. Cell Cycle. 15: 1787-95.

PMID: # 11259469  Soni, R. et al. 2001. J. Natl. Cancer Inst. 93: 436-446.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Soni Soni, R. et al. (PubMed 11259469) tested the inhibition efficacy of CINK4 (Cdk4/6 Inhibitor IV) on Cdk4 and its effects on tumor growth. Found that CINK4 selectively inhibited Cdk4 in vitro and slowed tumor growth of mice xenografted with HCT116 colon carcinoma cells. -SCBT Publication Review
Date published: 2015-04-16
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