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Angiogenesis Src PF477736

PF477736

Catalog No. T6028   CAS 952021-60-2
Synonyms: PF 477736, PF-477736, PF 00477736, PF-736,PF-00477736, PF-736,PF-00477736, PF-477736, PF 477736 PF 00477736

PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.

PF477736, CAS 952021-60-2
Pack Size Availability Price/USD Quantity
1 mg In stock 45.00
2 mg In stock 54.00
5 mg In stock 90.00
10 mg In stock 161.00
25 mg In stock 253.00
100 mg In stock 777.00
1 mL * 10 mM (in DMSO) In stock 96.00
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Purity 98.34%
Purity 98.34%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
Targets&IC50 c-Fms ,   Chk1 ,   Chk2 ,   VEGFR2 ,   Yes
Kinase Assay Binding assay: The assay is performed in a 96-well plate for 20 minutes at 30℃ in 0.1 mL of assay buffer containing 50 mM TRIS pH 7.5, 0.4 M NaCl, 4 mM PEP, 0.15 mM NADH, 28 units of lactate dehydrogenase/mL, 16 units of pyruvate kinase/mL, 3 mM DTT, 0.125 mM Syntide-2, 0.15 mM ATP and 25 mM magnesium chloride. Assays are initiated with 1 nM of CHK1 kinase domain. The inhibition of CHK1 activity is determined by measuring initial velocities in the presence of varying concentrations of PF-477736. The data is analyzed using Enzyme Kinetic and Excel software and fit to a kinetic model for competitive inhibition to obtain a Ki value. The kinase selectivity of PF-477736 is evaluated by screening the compound at 1 μM or 10 μM against a panel 2 of about 100 protein kinases.
Cell Research
The IC50 assay measures the antiproliferative effects of PF-477736 on p53-defective human cancer cell lines. Cells in each line are seeded in complete medium at an exponentially growing density in 96-well assay plate and allowed to attach for 16 hours. Serial dilutions of PF-477736 are then done, and appropriate controls are added to each plate. Cells are incubated with drug for 96 hours. After incubation, MTT working stock diluted in complete medium is added to each well, and cells are incubated for 4 hours. After centrifugation and supernatant removal, DMSO is added to each well and plates are read on SpectraMax plate reader at 540 nm. (Only for Reference)
Cell lines: HT29, Colo205, PC-3, MDA-MB-231 and K562 cells
Synonyms PF 477736 , PF-477736 , PF 00477736 , PF-736,PF-00477736 , PF-736,PF-00477736 , PF-477736 , PF 477736 PF 00477736
Purity 98.34%
Molecular Weight 419.48
Formula C22H25N7O2
CAS No. 952021-60-2

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 31.5 mg/mL (75 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

2% DMSO/40% PEG 300: 5 mg/mL

Citations

References and Literature
1. Blasina A, et al. Mol Cancer Ther, 2008, 7(8), 2394-2404. 2. Chakraborty J, et al. J Biol Chem, 2010, 285(43), 33104-33112. 3. Zhang C, et al. Clin Cancer Res, 2009, 15(14), 4630-4640. 4. Carrassa L, et al. Cell Cycle, 2012, 11(13), 2507-2517.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Apoptosis Compound Library Tyrosine kinase inhibitor library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library Cell cycle related Compound Library Anti-cancer Active Compound library Anti-cancer Drug library Drug Repurposing Library Target-Focused Phenotypic Screening Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-fibrosis Compound Library

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