R547 (mesylate)
R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively[1][2][3][4][5].
Product Specifications
CAS Number
869369-26-6
UNSPSC
12352005
Target
Apoptosis; CDK; GSK-3
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Stem Cell/Wnt
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/r547-mesylate.html
Smiles
O=S(N1CCC(NC2=NC(N)=C(C(C3=C(C(F)=CC=C3OC)F)=O)C=N2)CC1)(C)=O.CS(=O)(O)=O
Molecular Formula
C19H25F2N5O7S2
Molecular Weight
537.56
References & Citations
[1]Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N.Discovery of [4-Amino-2- (1-methanesulfonylpiperidin-4-ylamino) pyrimidin-5-yl] (2,3-difluoro-6- methoxyphenyl) methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.J Med Chem. 2006 Nov 2;49 (22) :6549-60.|[2]Bayés M, Rabasseda X, Prous JR.Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jul-Aug;29 (6) :427-37.|[3]Martin F, Thomson TM, Sewer A, Drubin DA, Mathis C, Weisensee D, Pratt D, Hoeng J, Peitsch MC.Assessment of network perturbation amplitudes by applying high-throughput data to causal biological networks.BMC Syst Biol. 2012 May 31;6:54.|[4]DePinto, Wanda et al In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials Molecular Cancer Therapeutics (2006), 5 (11), 2644-2658|[5]Jones, Clifford D.; Andrews, David M. Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors Bioorganic & Medicinal Chemistry Letters (2008), 18 (24), 6486-6489
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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