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PHA-665752

CAT: 0804-HY-11107-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-11107-01Size:5 mg
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Description
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM) . PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity[1][2].
CAS Number
477575-56-7
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; Autophagy; c-Met/HGFR
Type
Reference compound
Related Pathways
Apoptosis; Autophagy; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/PHA-665752.html
Concentration
10mM
Purity
99.85
Solubility
DMSO : 25 mg/mL (ultrasonic)
Smiles
O=C(C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)S(=O)(CC4=C(C=CC=C4Cl)Cl)=O)=O)=C1C)C)N5[C@H](CCC5)CN6CCCC6
Molecular Formula
C32H34Cl2N4O4S
Molecular Weight
641.61
Precautions
H302, H315, H319, H335
References & Citations
[1]Christensen JG, et al. 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.|[2]Ma PC. et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res. 2005 Mar 15;11 (6) :2312-9.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

Chemical Information

(3Z)-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-2H-indol-2-one

PHA-665752 is 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 ring 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). It has a role as an antineoplastic agent and a c-Met tyrosine kinase inhibitor. It is a secondary carboxamide, a tertiary carboxamide, a dichlorobenzene, a member of indolones, a sulfone, a N-acylpyrrolidine, a pyrrolecarboxamide and an enamide.

CAS Number477575-56-7
PubChem CID10461815
IUPAC Name(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one
Molecular FormulaC32H34Cl2N4O4S
Molecular Weight641.6
XLogP5
Topological Polar Surface Area111
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count7
Heavy Atom Count43
Formal Charge0
Complexity1180
SMILES
CC1=C(NC(=C1C(=O)N2CCC[C@@H]2CN3CCCC3)C)/C=C\4/C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O
InChI
InChI=1S/C32H34Cl2N4O4S/c1-19-29(35-20(2)30(19)32(40)38-14-6-7-21(38)17-37-12-3-4-13-37)16-24-23-15-22(10-11-28(23)36-31(24)39)43(41,42)18-25-26(33)8-5-9-27(25)34/h5,8-11,15-16,21,35H,3-4,6-7,12-14,17-18H2,1-2H3,(H,36,39)/b24-16-/t21-/m1/s1
InChIKey
OYONTEXKYJZFHA-SSHUPFPWSA-N
Chemical Structure
2D Structure
2D structure of (3Z)-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-2H-indol-2-one
CAS: 477575-56-7
CID: 10461815
Formula: C32H34Cl2N4O4S
MW: 641.6
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight641.6
XLogP35
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count7
Exact Mass640.1677821
Monoisotopic Mass640.1677821
Topological Polar Surface Area111 Ų
Heavy Atom Count43
Formal Charge0
Complexity1180
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count1
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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