PF 477736

PF 477736 Basic information
target
Product Name:PF 477736
Synonyms:PF 477736;PF-00477736;PF-736;(αR)-α-AMino-N-[5,6-dihydro-2-(1-Methyl-1H-pyrazol-4-yl)-6-oxo-1H-pyrrolo[4,3,2-ef][2,3]benzodiazepin-8-yl]cyclohexaneacetaMide;PF 477736(PF-0044736);(2R)-2-aMino-2-cyclohexyl-N-[2-(1-Methyl-1H-pyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.0^{4,13}]trideca-1,4(13),5,7,11-pentaen-6-yl]acetaMide;PF0044736;PF-0044736
CAS:952021-60-2
MF:C22H25N7O2
MW:419.49
EINECS:
Product Categories:Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals
Mol File:952021-60-2.mol
PF 477736 Structure
PF 477736 Chemical Properties
density 1.56
storage temp. 2-8°C
solubility DMSO: ≥20mg/mL
form powder
pka11.79±0.20(Predicted)
color yellow
InChIKeyNDEXUOWTGYUVGA-LJQANCHMSA-N
Safety Information
WGK Germany 3
MSDS Information
PF 477736 Usage And Synthesis
targettarget of PF 477736
DescriptionCheckpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2. When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.
UsesP293850 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage.
UsesCheckpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2. When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.[Cayman Chemical]
UsesPF-477736 has been used as a checkpoint protein 1 (CHK1) inhibitor to study the effect of CHK1 in cell cycle regulation in primary breast and lung primary epithelial cells.
DefinitionChEBI: PF-00477736 is a diazepinoindole that is 8-amino-4,5-dihydro-6H-[1,2]diazepino[4,5,6-cd]indol-6-one which is substituted at position 2 by a 1-methylpyrazol-4-yl group and in which the amino group at position 8 has undergone condensation with the carboxy group of (2R)-2-cyclohexylglycine to give the corresponding carboxamide. It is an inhibitor of checkpoint kinase 1 (Chk 1). It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor and an antineoplastic agent. It is an amino acid amide, a member of pyrazoles and a diazepinoindole.
Biochem/physiol ActionsPF-477736 may be effectively used to resensitize platinum resistant ovarian cancer cells. PF-477736 alone or in combination with other chemotherapeutic agents may be used to treat triple-negative breast cancer.
storageStore at +4°C
references[1] blasina a1, hallin j, chen e, arango me, kraynov e, register j, grant s, ninkovic s, chen p, nichols t, o'connor p, anderes k. breaching the dna damage checkpoint via pf-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. mol cancer ther. 2008 aug;7(8):2394-404.
PF 477736 Preparation Products And Raw materials
AZD-1208 1H-Indole-2-carboxamide, 4-methoxy-N-[(1S)-3-methyl-1-[[[(1S)-2-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-3-(phosphonooxy)propyl]amino]carbonyl]butyl]- PF-04691502 [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate PF-05212384 PF-5190457 PF-06882961 PF 573228 PF-3084014 VE 822 PF 04995274 PF 3644022 PF-06447475 PF-06424439 AZD7762 MK-8776 (SCH 900776) LY2603618 Sunitinib

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