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ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >protein tyrosine kinase >(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE Structure
CAS No.
477575-56-7
Chemical Name:
(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE
Synonyms
CS-40;PHA 665752;PHA-665752/PHA665752;PHA-665752 c-Met Inhibitor;(R,Z)-5-((2,6-Dichlorobenzyl)sulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin;(R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one;(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE;2H-Indol-2-one, 5-[[(2,6-dichlorophenyl)methyl]sulfonyl]-3-[[3,5-dimethyl-4-[[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]carbonyl]-1H-pyrrol-2-yl]methylene]-1,3-dihydro-, (3Z)-;(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE USP/EP/BP;(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE PHA 665752
CBNumber:
CB72448634
Molecular Formula:
C32H34Cl2N4O4S
Molecular Weight:
641.61
MOL File:
477575-56-7.mol
MSDS File:
SDS
Modify Date:
2023/9/4 15:51:00
Request For Quotation

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE Properties

Boiling point 890.2±65.0 °C(Predicted)
Density 1.404
storage temp. Sealed in dry,2-8°C
solubility DMSO: ≥20mg/mL
form powder
pka 11.39±0.20(Predicted)
color light yellow to light brown
optical activity [α]/D +50 to +70°, c = 0.2 in methanol

SAFETY

Risk and Safety Statements

WGK Germany  3

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) PZ0147 PHA-665752 hydrate ≥98% (HPLC) 477575-56-7 5MG ₹15891.1 2022-06-14 Buy
Sigma-Aldrich(India) PZ0147 PHA-665752 hydrate ≥98% (HPLC) 477575-56-7 25MG ₹58844.7 2022-06-14 Buy
Product number Packaging Price Buy
PZ0147 5MG ₹15891.1 Buy
PZ0147 25MG ₹58844.7 Buy

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE Chemical Properties,Uses,Production

Description

The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers. PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM). It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC50s = 18-50 nM). It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines. In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.

Chemical Properties

Yellow powder crystal

Uses

PHA-665752 ia a c-Met kinase inhibitor. PHA-665752 is ATP-competitive, an active-site inhibitor with greater than 50-fold selectivity for c-Met vs a panel of tyrosine and serine-threonine kinases.

Definition

ChEBI: A member of the class of indolones that is 1,3-dihydro-2H-indol-2-one which is substituted by a (2,6-dichlorobenzyl)sulfonyl group at position 5 and by a (1H-pyrrol-2-yl)methylidene group at position 2, the pyrrole rin of which is substituted by methyl groups at positions 3 and 5, and by a [2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]carbonyl group at position 4 (the Z,R isomer).

Biological Activity

Potent, selective and ATP-competitive inhibitor of MET kinase (IC 50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB α , p38 α , MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE Preparation Products And Raw materials

Raw materials

Preparation Products

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE Suppliers

Global( 144)Suppliers
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A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32760 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29898 58 Inquiry
Chongqing Chemdad Co., Ltd +86-023-6139-8061 +86-86-13650506873 China 39916 58 Inquiry
CONIER CHEM AND PHARMA LIMITED +8618523575427 China 49391 58 Inquiry
Dideu Industries Group Limited +86-29-89586680 +86-15129568250 China 24639 58 Inquiry
Zhejiang J&C Biological Technology Co.,Limited +1-2135480471 +1-2135480471 China 10522 58 Inquiry
changzhou huayang technology co., ltd +8615250961469 China 9827 58 Inquiry
InvivoChem +1-708-310-1919 +1-13798911105 United States 6393 58 Inquiry
Nantong HI-FUTURE Biology Co., Ltd. +undefined18051384581 China 3136 58 Inquiry
Supplier Advantage
A.J Chemicals 58
ATK CHEMICAL COMPANY LIMITED 60
career henan chemical co 58
Chongqing Chemdad Co., Ltd 58
CONIER CHEM AND PHARMA LIMITED 58
Dideu Industries Group Limited 58
Zhejiang J&C Biological Technology Co.,Limited 58
changzhou huayang technology co., ltd 58
InvivoChem 58
Nantong HI-FUTURE Biology Co., Ltd. 58

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE Spectrum

(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE(477575-56-7)1HNMR

477575-56-7((2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE)Related Search:

PHA-848125 Bortezomib Tivantinib (ARQ 197) SU 11274 Veliparib
Crizotinib Olaparib PHA-665752 R)-N-METHYL-2-PYRROLIDIN-1-YLMETHYL-PYRROLIDINE p-(ethylsulfonyl)-anilin
1-(Cloromethyl)-4,5-dihydro-1H-imidazole hydrochloride SU 5416 (R)-(-)-1-(2-Pyrrolidinylmethyl)pyrrolidine
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PHA 665752 (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE PHA 665752 PHA-665752/PHA665752 (R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one PHA 665752 (2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine (R,Z)-5-((2,6-Dichlorobenzyl)sulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE USP/EP/BP 2H-Indol-2-one, 5-[[(2,6-dichlorophenyl)methyl]sulfonyl]-3-[[3,5-dimethyl-4-[[(2R)-2-(1-pyrrolidinylmethyl)-1-pyrrolidinyl]carbonyl]-1H-pyrrol-2-yl]methylene]-1,3-dihydro-, (3Z)- CS-40 PHA-665752 c-Met Inhibitor 477575-56-7 C32H34Cl2N4O4S Inhibitors