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ChemicalBook > CAS DataBase List > PF 477736

PF 477736

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Product Name
PF 477736
CAS No.
952021-60-2
Chemical Name
PF 477736
Synonyms
PF-736;CS-237;PF0044736;PF 477736;PF0477736;PF-0044736;PF-00477736;PF-736,PF-00477736;PF-477736 PF477736;PF 477736 USP/EP/BP
CBNumber
CB02535690
Molecular Formula
C22H25N7O2
Formula Weight
419.49
MOL File
952021-60-2.mol
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PF 477736 Property

Density 
1.56
storage temp. 
2-8°C
solubility 
DMSO: ≥20mg/mL
form 
powder
pka
11.79±0.20(Predicted)
color 
yellow
InChIKey
NDEXUOWTGYUVGA-LJQANCHMSA-N
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0186
Product name
PF-477736
Purity
≥98% (HPLC)
Packaging
5mg
Price
$133
Updated
2024/03/01
Sigma-Aldrich
Product number
PZ0186
Product name
PF-477736
Purity
≥98% (HPLC)
Packaging
25mg
Price
$432
Updated
2024/03/01
Cayman Chemical
Product number
17859
Product name
PF-477736
Purity
≥98%
Packaging
5mg
Price
$106
Updated
2024/03/01
Cayman Chemical
Product number
17859
Product name
PF-477736
Purity
≥98%
Packaging
10mg
Price
$198
Updated
2024/03/01
Cayman Chemical
Product number
17859
Product name
PF-477736
Purity
≥98%
Packaging
25mg
Price
$414
Updated
2024/03/01
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PF 477736 Chemical Properties,Usage,Production

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Description

Checkpoint 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.

Uses

Checkpoint 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]

Uses

PF-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.

Uses

P293850 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.

Definition

ChEBI: 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 Actions

PF-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.

storage

Store 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

Raw materials

Preparation Products

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PF 477736 Suppliers

Canada 1 China 87 United Kingdom 2 United States 18 Global 108
Novachemistry
Tel
44-20819178-90 02081917890
Fax
(0)2080432064
Email
info@novachemistry.com
Country
United Kingdom
ProdList
4381
Advantage
58
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77
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View Lastest Price from PF 477736 manufacturers

Career Henan Chemical Co
Product
PF 477736 952021-60-2
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100KG
Release date
2018-08-20

952021-60-2, PF 477736Related Search:

PF-05089771 (tosylate) PF-06424439 PF-06447475 PF 3644022 PF 04995274 PF-3084014 PF 573228 PF-06882961 PF-5190457 PF-05212384 [(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-04691502 Sunitinib LY2603618 MK-8776 (SCH 900776) AZD7762 VE 822 PF-06650833

  • 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
  • (alphaR)-alpha-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
  • Cyclohexaneacetamide, 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]-, (αR)-
  • PF-736,PF-00477736
  • (alphaR)-alpha-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
  • (2R)-2-Amino-2-cyclohexyl-N-[2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-acetamide
  • 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
  • PF0477736
  • (R)-2-AMINO-2-CYCLOHEXYL-N-[2-(1-METHYL-1H-PYRAZOL-4-YL)-6-OXO-5,6-DIHYDRO-1H-[1,2]DIAZEPINO[4,5,6-CD]INDOL-8-YL]-ACETAMIDE
  • (R)-2-Amino-2-cyclohexyl-N-(2-(1-methyl-1H-pyrazol-4-yl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4
  • NDEXUOWTGYUVGA-LJQANCHMSA-N
  • CS-237
  • PF 477736;PF-477736;PF477736
  • PF 477736 - PF 00477736
  • PF 477736 USP/EP/BP
  • PF-477736 PF477736
  • (R)-2-Amino-2-cyclohexyl-N-(5-(1-methyl-1H-pyrazol-4-yl)-1-oxo-2,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide
  • PF 477736, 10 mM in DMSO
  • 952021-60-2
  • 952021-60-3
  • C22H25N7O22ClH
  • Amines
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pfizer Compounds
  • Pharmaceuticals