R547

Item no.	HY-10014-100mg
Manufacturer	MedChem Express
CASRN	741713-40-6
Amount	100 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 1 mg 25 mg 500 mg 50 mg 5 mg
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Colorectal Cancer Breast Cancer
Type	Inhibitors
Specific against	other
Purity	99.57
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
Smiles	O=S(N1CCC(NC2=NC(N)=C(C(C3=C(C(F)=CC=C3OC)F)=O)C=N2)CC1)(C)=O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	R 547, R-547
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	Apoptosis; CDK; GSK-3
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	441.45
Product Description	R547 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].
Manufacturer - Research Area	Cancer
Solubility	10 mM in DMSO
Manufacturer - Pathway	Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Stem Cell/Wnt
Isoform	CDK1; CDK2; CDK3; CDK4; CDK5; CDK6; CDK7; GSK-3α; GSK-3β
Clinical information	Phase 1

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HY-10014-100mg-safety-datasheet.pdf