(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
- Product 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
- 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
- Formula Weight
- 641.61
- MOL File
- 477575-56-7.mol
(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 Property
- Boiling point:
- 890.2±65.0 °C(Predicted)
- Density
- 1.404
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: ≥20mg/mL
- pka
- 11.39±0.20(Predicted)
- form
- powder
- color
- light yellow to light brown
- optical activity
- [α]/D +50 to +70°, c = 0.2 in methanol
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- PZ0147
- Product name
- PHA-665752 hydrate
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $155
- Updated
- 2024/03/01
- Product number
- PZ0147
- Product name
- PHA-665752 hydrate
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $580
- Updated
- 2024/03/01
- Product number
- 14703
- Product name
- PHA 665752
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 14703
- Product name
- PHA 665752
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $77
- Updated
- 2024/03/01
- Product number
- 14703
- Product name
- PHA 665752
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $134
- Updated
- 2024/03/01
(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,Usage,Production
Description
The c-
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.
Biochem/physiol Actions
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.
in vivo
pha-665752 inhibits c-met phosphorylation as well as tumor growth in both s114 and gtl-16 implanted xenograft athymic mice [1].
storage
Store at +4°C
References
[1] christensen jg1, schreck r, burrows j, kuruganti p, chan e, le p, chen j, wang x, ruslim l, blake r, lipson ke, ramphal j, do s, cui jj,cherrington jm, mendel db. a selective small molecule inhibitor of c-met kinase inhibits c-met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. cancer res. 2003 nov 1;63(21):7345-55.
(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
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View Lastest Price from (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 manufacturers
- Product
- (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
- Price
- US $3.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2019-08-07