Newblue-CHEM - R547

Min.Order / FOB Price:Get Latest Price

1 Kilogram	FOB Price: USD 1000.0000

1 Kilogram

FOB Price: USD 1000.0000

Min.Order :1 Kilogram
Purity: 99%
Payment Terms : L/C,D/A,D/P,T/T,Other

Keywords

Methanone,[4-amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxy 741713-40-6 R547

Quick Details

Appearance:white powder
Application:Organic Chemicals
PackAge:As required
ProductionCapacity:10|Metric Ton|Month
Storage:room tempurature
Transportation:As per MSDS

Superiority:

Our company engages in Sodium Tripolyphosphate (STPP) and Sodium Hexametabphosphate (SHMP) production; development of noble metal catalysts, synthesis of electronic chemical materials and general chemicals Imp&Exp trading business. The company is located in Zhengzhou High-tech Development Zone with import and export license. We passed ISO 9001:2008 in 2009, and won "High-tech Enterprise" by provincial government in 2013. Our STPP and SHMP has reached an annual output of 30000 tons and has successfully passed SGS, CIQ audits on many occasions.

In 2011 we entered the fine chemical market of Noble Metal Catalyst ,Organic Phosphine Ligands and OLED intermediates.With the joint efforts of our senior experts and professional technicians, Newblue has developed more than 500 compounds, which are widely used in the fields of production and life science. The objective of the company is to put quality first and put our customer’s needs first - the satisfaction of our customers is the company's ultimate goal. Improving product quality and service level is our responsibility, and creating more value for our customer’s is our purpose. We are constantly striving to make Henan Newblue a leading chemical supplier, and hope to create a better future with you.

Details:

R547 Basic information

Description In vitro In vivo

Product Name: R547

Synonyms: [4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547);R547;[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone;Ro 4584820;[4-aMino-2-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-5-pyriMidinyl](2;3-difluoro-6-Methoxyphenyl)-;R547(Ro 4584820);5-[(2,3-difluoro-6-Methoxyphenyl)carbonyl]-2-N-(1-Methanesulfonylpiperidin-4-yl)pyriMidine-2,4-diaMine

CAS: 741713-40-6

MF: C18H21F2N5O4S

MW: 441.45

EINECS:

Product Categories: Inhibitors

Mol File: 741713-40-6.mol

R547 Structure

R547 Chemical Properties

density 1.49

Safety Information

MSDS Information

R547 Usage And Synthesis

Description R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

In vitro R547 identified as a diaminopyrimidine compound, which is a potent and selective ATP-competitive CDK inhibitor. R547 effectively inhibits CDK1/cyclinB, CDK2/cyclinE, and CDK4/cyclinD1(Ki=1-3nM) and is inactive(Ki>5,000nM) against a panel of >120 unrelated kinases. R547 effectively inhibits the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50s <0.60 μM. R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest, suggesting a potential pharmaco dynamics marker for clinical use. R547 inhibits the proliferation of tumor cell lines and is active in all 19 cell lines tested irrespective of tissue of origin, multidrug resistance (MDR), p53, or retinoblastoma status. R547 possessing both 5-and 6-fluoro substitution culminated in an Inhibitor with low, single-digit nanomolar potency against the CDKs(Ki=0.001,0.003,and 0.001 μM for CDK1,CDK2, and CDK4,respectively) and excellent cellular potency (IC50=0.08 μM,HCT116 cell line).

In vivo R547 administered with oral and i.v. dosing in multiple established human tumor significantly inhibits tumor activity(P < 0.01). R547 administered orally at dose of 40 mg/kg daily in colon, lung, breast, prostate, and melanoma human tumor xenograft models shows significant TGI (79-99%). R547 is equally efficacious (TGI, 61-95%) when dosed with 40 mg/kg i.v. once weekly. These doses of R547 are not toxic and did not result in body weight loss. R547 does not show signs of overt toxicity during the course of the 3-week study and any gross pathology at necropsies done at the end of the studies.R547 inhibits tumor growth up to 95% in the HCT116 human colorectal tumor xenograft model in nude mice . R547 causes significant TGI in all of the models tested when dosed orally and i.v. at or below the maximum tolerated dose. R547 inhibits phosphorylation of retinoblastoma protein in tumors at the efficacious exposures in tumor xenograft models, providing a pharmacodynamic biomarker for clinical use. R547 reported here suggests that this is a promising molecule for evaluation in the treatment of solid tumors.

R547 Preparation Products And Raw materials

View All

Visit Store