PF 477736

Name: PF 477736
Brand: Tocris Bioscience
SKU: 4277

Tocris Bioscience, part of Bio-Techne | Catalog # 4277

Citations (8)

COA / SDS

Selective Chk1 inhibitor

Key Product Details

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
Purity:	≥99%
Molecular Weight:	419.48 kDa

View Full Technical Details for PF 477736

Technical Data
Citations

Biological Activity for PF 477736

PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (K_i 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.

Technical Data for PF 477736

M. Wt	419.48 kDa
Formula	C₂₂H₂₅N₇O₂
Storage	Store at +4°C
Purity	≥99%
CAS Number	952021-60-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 477736

Solubility

Soluble Soluble to 75 mM in DMSO

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References for PF 477736

References are publications that support the biological activity of the product.

S Liu, Y Liu, K Minami, A Chen, Q Wan, Y Yin, L Gan, A Xu, N Matsuura, M Koizumi, Y Liu, S Na, J Li, H Nakshatri, BY Li, H Yokota Inhibiting checkpoint kinase 1 protects bone from bone resorption by mammary tumor in a mouse model Oncotarget, 2018;9(10):9364-9378. 2018 PMID: 29507695
Ashwell and Zabludoff DNA damage detection and repair pathways - recent advances with inhibitors of checkpoint kinases in cancer therapy. Clin.Cancer Res., 2008;14:4032 PMID: 18593978
Blasina et al. Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol.Cancer Ther., 2008;7:2394 PMID: 18723486
Zhang et al. PF-00477736 mediates checkpoint kinase 1 signaling pathways and potentiates docetaxel-induced efficacy in xenografts. Clin.Cancer Res., 2009;15:4630 PMID: 19584159