R&D Systems Inc. Tocris Bioscience Boston Biochem

PF 477736

Cat. No. 4277

PF 477736 C22H25N7O2 [952021-60-2]

Price and Availability

For PF 477736 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Alternative Name: PF-0044736

Chemical Name: (R)-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

Biological Activity

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. Enhances docetaxel (Cat. No. 4056) efficacy in tumor cells and xenografts.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
419.48
Formula:
C22H25N7O2
Solubility:
Soluble to 75 mM in DMSO
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
952021-60-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

Ashwell and Zabludoff (2008) DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy. Clin.Cancer Res. 14 4032. PMID: 18593978.

Blasina et al (2008) Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol.Cancer Ther. 7 2394. PMID: 18723486.

Zhang et al (2009) PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts. Clin.Cancer Res. 15 4630. PMID: 19584159.

If you know of a relevant citation for this product please let us know.

Keywords: PF 477736, supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Guide

Highlights over 350 products for cancer research. Request a copy or view PDF today.

divider line

Kinases Product Listing

Kinases Product Listing

Highlights over 350 products for kinase research. Request a copy or view PDF today.

divider line

Kinase Inhibitor Toolbox

80 Kinase inhibitors
pre-dissolved in DMSO

Kinase Inhibitor Toolbox

Includes many of the latest kinase inhibitors to become commercially available. Covers a wide range of kinase targets including EGFR, MAPK and CDK.

divider line

Checkpoint Kinases & the DNA Damage Response

Written by Michelle D. Garrett and Ian Collins

Cell Cycle Kinases Poster

A summary of the response of the checkpoint kinase signaling network to DNA damage, including activation of DNA repair, cell-cycle arrest, senescence and apoptosis.

divider line

New Product Guide

NPG

Highlights 150 new products added in the second half of 2014. View PDF today.

divider line

New Products in this Area

CKI 7 dihydrochloride

CK1 inhibitor

T 5601640

Selective LIMK2 inhibitor; antitumor

3PO

PFKFB3 inhibitor; antiangiogenic

CHR 6494 trifluoroacetate

Potent and selective haspin kinase inhibitor

UNC 3230

Potent and selective PIP5K1C inhibitor; antinociceptive

trans-ISRIB

Integrated stress response (ISR) inhibitor

trans-ISRIB

Integrated stress response (ISR) inhibitor

BMS 509744

Potent and selective ITK inhibitor

WZ 4003

Potent and selective NUAK1/2 inhibitor

TC-S 7010

Potent and selective Aurora kinase A inhibitor

Bryostatin 2

Protein kinase C activator

ZLN 024 hydrochloride

Allosteric AMPK activator

Temsirolimus

mTOR inhibitor; antitumor

KN 93 phosphate

CaM kinase II inhibitor; water soluble version of KN 93 (Cat. No. 1278).

ETP 45835 dihydrochloride

Mnk1 and Mnk2 inhibitor

Bryostatin 3

Potent protein kinase C activator

GKA 50

Glucokinase activator

Sign-up for new product e-alerts
divider line

Bio-Techne Events

DPG 2015

11th Göttingen Meeting of the German Neuroscience Society

March 18 - 21, 2015

Göttingen University, Germany

Booth: 39