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ChemicalBook >> CAS DataBase List >>[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) Structure
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) structure
CAS No.
741713-40-6
Chemical Name:
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)
Synonyms
R547;CS-238;Ro 4584820;R547(Ro 4584820);R547 >=98% (HPLC);R547 Ro-4584820 R-547;3-difluoro-6-Methoxyphenyl)-;[4-aMino-2-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-5-pyriMidinyl](2;(4-Amino-2-((1-(methylsulfonyl)piperidin-4-yl)amino)pyrimidin-5-yl)(2,3-difluoro-6-methoxyphen;5-[(2,3-difluoro-6-Methoxyphenyl)carbonyl]-2-N-(1-Methanesulfonylpiperidin-4-yl)pyriMidine-2,4-diaMine
CBNumber:
CB41562444
Molecular Formula:
C18H21F2N5O4S
Molecular Weight:
441.45
MDL Number:
MFCD09970629
MOL File:
741713-40-6.mol
MSDS File:
SDS
Last updated:2024-07-02 08:55:08
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[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) Properties

Boiling point 703.7±70.0 °C(Predicted)
Density 1.49
storage temp. Store at -20°C
solubility Soluble in DMSO
form crystalline solid
pka 4.22±0.10(Predicted)
color White to off-white
FDA UNII T61871RKRI

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) price More Price(17)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 17905 R547 ≥98% 741713-40-6 1mg $120 2024-03-01 Buy
Cayman Chemical 17905 R547 ≥98% 741713-40-6 5mg $537 2024-03-01 Buy
Tocris 5494 R547 ≥98%(HPLC) 741713-40-6 10 $235 2021-12-16 Buy
ApexBio Technology A8642 R547 741713-40-6 10mg $270 2021-12-16 Buy
Axon Medchem Axon1983 R547 99% 741713-40-6 2x25mg $484 2021-12-16 Buy
Product number Packaging Price Buy
17905 1mg $120 Buy
17905 5mg $537 Buy
5494 10 $235 Buy
A8642 10mg $270 Buy
Axon1983 2x25mg $484 Buy

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) Chemical Properties,Uses,Production

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.

Description

Cyclin-dependent kinases (Cdks) are critical positive regulators of cell cycle progression and cellular transcription whose dysregulation can lead to the development of cancer. R547 is a diaminopyrimidine compound that inhibits Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1 (Kis = 1-3 nM). It is inactive against a panel of more than 120 unrelated kinases (Kis > 5 μM). R547 inhibits tumor cell proliferation (IC50s ≤ 0.6 μM in vitro), inducing cell cycle arrest at G1 and G2 phases and apoptosis as well as reducing phosphorylation of the retinoblastoma protein. It also demonstrates antitumor activity in vivo in various human tumor xenograft models.

target

CDK4/CyclinD1

storage

Store at +4°C

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) Preparation Products And Raw materials

Raw materials

Preparation Products

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) Suppliers

Global( 108)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32760 60
Hubei xin bonus chemical co. LTD 		86-13657291602 linda@hubeijusheng.com CHINA 22968 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 49391 58
career henan chemical co 		+86-0371-86658258 +8613203830695 factory@coreychem.com China 29826 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 25808 58
Hefei Hirisun Pharmatech Co., Ltd 		+8615056975894 shawn@hirisunpharm.com CHINA 9923 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10522 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58
Coresyn Pharmatech Co., Ltd. 		+86-571-86626709 +86-18157142896 cbc@coresyn.com China 9991 58
TargetMol Chemicals Inc. 		+1-781-999-5354 support@targetmol.com United States 19973 58
Supplier Advantage
ATK CHEMICAL COMPANY LIMITED 		60
Hubei xin bonus chemical co. LTD 		58
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
Dideu Industries Group Limited 		58
Hefei Hirisun Pharmatech Co., Ltd 		58
Zhejiang J&C Biological Technology Co.,Limited 		58
InvivoChem 		58
Coresyn Pharmatech Co., Ltd. 		58
TargetMol Chemicals Inc. 		58

View Lastest Price from [4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) pictures 2019-12-31 [4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)
741713-40-6
 US $1.00 / g 1g 99% 200kg Career Henan Chemical Co

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) Spectrum

[4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547)(741713-40-6)1HNMR

741713-40-6([4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547))Related Search:

Sulfanilamide AT7519 Selumetinib CAL-101 (2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol
Rapamycin Abemaciclib mesylate (LY2835219) 2,4-Diamino-5-(3-fluorobenzyl)pyrimidine 2-(ISOPROPYLAMINO)PYRIMIDINE-5-CARBALDEHYDE 2'-FLUORO-6'-HYDROXYACETOPHENONE
Benzaldehyde, 2,3-difluoro-6-hydroxy- (9CI) 2,3-DIFLUORO-6-METHOXYBENZALDEHYDE R547 2'-FLUORO-6'-METHOXYACETOPHENONE

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[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 (4-Amino-2-{[1-(methylsulfonyl)-4-piperidinyl]amino}-5-pyrimidinyl)(2,3-difluoro-6-methoxyphenyl)methanone (4-Amino-2-((1-(methylsulfonyl)piperidin-4-yl)amino)pyrimidin-5-yl)(2,3-difluoro-6-methoxyphen CS-238 Methanone, [4-amino-2-[[1-(methylsulfonyl)-4-piperidinyl]amino]-5-pyrimidinyl](2,3-difluoro-6-methoxyphenyl)- R547 >=98% (HPLC) [4-Amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R 547) USP/EP/BP R547 Ro-4584820 R-547 741713-40-6 C18H21F2N5O4S Inhibitors