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Tocris/PF 477736/4277/10/10 mg

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货号: 4277/10

品牌: Tocris

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Description: Selective Chk1 inhibitor

Alternative Names: 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

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 477736 is reviewed on the chemical probes website.

Compound Libraries

PF 477736 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	419.48
Formula	C₂₂H₂₅N₇O₂
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	952021-60-2
PubChem ID	16750408
InChI Key	YFNWWNRZJGMDBR-LJQANCHMSA-N
Smiles	O=C([C@H](N)C4CCCCC4)NC1=CC3=C(C(C=NNC3=O)=C(C5=CN(C)N=C5)N2)C2=C1

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.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	31.46	75

Preparing Stock Solutions

The following data is based on the product molecular weight 419.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.38 mL	11.92 mL	23.84 mL
5 mM	0.48 mL	2.38 mL	4.77 mL
10 mM	0.24 mL	1.19 mL	2.38 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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

Keywords: PF 477736, supplier, pfizer, PF477736, checkpoint, kinases, chk1, selective, inhibitors, inhibits, dna, damage, cell, cycle, arrest, abrogates, PF0044736, PF-0044736, Checkpoint, Kinases, Checkpoint, Control, Kinases, Checkpoint, Kinases, Tocris Bioscience

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