Home Tools
Log in

PF 477736

Catalog No. T6028   CAS 952021-60-2
Synonyms: PF 00477736, PF477736, PF-736,PF-00477736, PF-477736

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PF 477736, CAS 952021-60-2
Please contact us for prices and availability for the specification of product you are interested at.
Product consultation
Get quote
Purity: 98%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
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 Chk2:47 nM(Ki), Chk1:0.49 nM(Ki), YES:14 nM(Ki), VEGFR2:8 nM(Ki), FMS:10 nM(Ki)
In vitro PF-477736 (128 nM) abrogates the camptothecin-induced DNA damage checkpoint in a dose-dependent manner in CA46 and HeLa cells. PF-477736 effectively abrogates the gemcitabine-induced S-phase arrest with a corresponding increase in apoptotic cell populations in HT29 cells. PF-477736 (540 nM) enhances gemcitabine-induced cytotoxicity in a time- and dose-dependent manner in HT29 cells. PF-477736 potentiates the growth-inhibitory activity of a panel of chemotherapeutic agents across a broad spectrum of p53-deficient human cancer cell lines in the MTT assay. Addition of PF-477736 (360 nM) to gemcitabine-arrested cells induces a dramatic increase in the intensity of H2AX phosphorylation, reflecting a greater number of γ-H2AX molecules near sites of DNA damage. [1] PF-477736 (0.5 nM) selectively blocks p73 and P53 phosphorylation in presence of curcumin in HL-60 cells. [2] PF-477736 (360 nM) suppresses docetaxel-induced phosphorylation of histone H3 (Ser10) and Cdc25C (Ser216) and potentiates apoptosis in COLO205 cells. [3] PF-477736 (250 nM) combined with MK-1775 has marked synergistic cytotoxic activity in OVCAR-5 cells. PF-477736 (250 nM) combined with MK-1775 causes accumulation of cells with a DNA content between 2N and 4N in OVCAR-5 cells. PF-477736 (250 nM) combined with MK-1775 causes premature mitosis before the end of DNA replication, with damaged DNA leading to apoptotic cell death in OVCAR-5 cells. [4]
In vivo PF-477736 (4 mg/kg i.v.) results in terminal half-life (T1/2) of 2.9 hours, AUC of 5.72 μg×hr/mL and CLp of 11.8 mL/min/kg in rats. PF-477736 dose-dependently enhances the antitumor activity of a maximum tolerated dose of gemcitabine in the Colo205 xenograft mouse model. PF-477736 (12 mg/kg) induces an increase in the phosphorylation of histone H3 (Ser10) and of phospho-histone H2AX in the Colo205 xenograft mouse model. [1] PF-477736 (15 mg/kg i.p.) enhances docetaxel induced tumor growth inhibition and tumor growth delay in COLO205 and MDA-MB-231 xenograft models. [3] PF 477736 (10 mg/kg once daily i.p.) combined with MK-1775 (30 mg/kg twice a day oral) leads to greater tumor growth inhibition in mice bearing OVCAR-5 xenografts. [4]
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)
Synonyms PF 00477736, PF477736, PF-736,PF-00477736, PF-477736
Molecular Weight 419.489
Formula C22H25N7O2
CAS No. 952021-60-2


Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 31.5 mg/mL (75 mM)

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

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:
Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Cell Cycle Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Apoptosis Compound Library Angiogenesis related Compound Library

Related Products

Related compounds with same targets
Tripolin A CCT129202 SCH-1473759 L 888607 Racemate LY3295668 Centrinone-B Barasertib Aurora B inhibitor 1

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Average weight of animals
Dosing volume per animal
Number of animals
Step Two: Enter the in vivo formulation
% Tween 80
% ddH2O
Calculate Reset


Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box


Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box


Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.


Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.


PF 477736 952021-60-2 表观遗传 蛋白酪氨酸激酶 凋亡 细胞周期 血管生成 Aurora Kinase CDK c-Fms Chk c-RET FGFR FLT Src VEGFR PF477736 CSF-1R PF-00477736 FLT3 CSF-1 receptor Cluster of differentiation antigen 135 PF 00477736 Fibroblast growth factor receptor Gemcitabine PF00477736 Checkpoint Kinase (Chk) Vascular endothelial growth factor receptor CSF1R Inhibitor colony stimulating factor 1 receptor PF-477736 Chk1 Chk2 PF-736,PF-00477736 Fms like tyrosine kinase 3 RET Cyclin dependent kinase antitumor inhibit CD135 inhibitor