R-547 ( R547 )

Catalog No. M15831 CAS No. 741713-40-6

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Datasheet

HNMR

HPLC

MSDS

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Product Name

R-547
Note

Research use only, not for human use.
Brief Description

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

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
Synonyms

R547
Pathway

Angiogenesis
Target

CDK
Recptor

CDK1/CyclinB; CDK2/CyclinE; CDK4/CyclinD1; PKA
Research Area

Cancer
Indication

Solid Tumors

CAS Number

741713-40-6
Formula Weight

441.45
Molecular Formula

C18H21F2N5O4S
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

O=C(C1=CN=C(NC2CCN(S(=O)(C)=O)CC2)N=C1N)C3=C(OC)C=CC(F)=C3F
Chemical Name

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

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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