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R547

Chemical Structure : R547

CAS No.: 741713-40-6

R547 (CDK inhibitor R547)

Catalog No.: PC-42067Not For Human Use, Lab Use Only.

R547 is a potent, selective and ATP-competitive CDK inhibitor with Ki of 1/3/1 nM for CDK1/2/4, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

R547 is a potent, selective and ATP-competitive CDK inhibitor with Ki of 1/3/1 nM for CDK1/2/4, respectively.
R547 has no activity against a large panel of serine/threonine and tyrosine kinases.
R547 inhibits the growth of various human tumor cell lines (HCT116 cell line IC50=80 nM), blocks G1 and G2 phases, induces apoptosis and reduces phosphorylation of Rb.
R547 demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice.

Physicochemical Properties

M.Wt 441.4522
Formula C18H21F2N5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Methanone, [4-amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)-

References

1. Chu XJ, et al. J Med Chem. 2006 Nov 2;49(22):6549-60.

2. DePinto W, et al. Mol Cancer Ther. 2006 Nov;5(11):2644-58.

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