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R-547

Chemical Structure : R-547

CAS No.: 741713-40-6

R-547 (R547)

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

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

A potent, selective and ATP-competitive CDK inhibitor with Ki of 1/3/1 nM for CDK1/2/4, respectively; has no activity against a large panel of serine/threonine and tyrosine kinases; 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; demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice.

Solid Tumors

Phase 1 Discontinued

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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