1. Cell Cycle/DNA Damage
    Protein Tyrosine Kinase/RTK
    Epigenetics
  2. Checkpoint Kinase (Chk)
    VEGFR
    Src
    c-Fms
    Aurora Kinase
    FGFR
    FLT3
    RET
    CDK
  3. PF 477736

PF 477736 (Synonyms: PF 00477736)

Cat. No.: HY-10032 Purity: 99.21%
Handling Instructions

PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

For research use only. We do not sell to patients.

PF 477736 Chemical Structure

PF 477736 Chemical Structure

CAS No. : 952021-60-2

Size Stock
10 mM * 1 mL in DMSO Get quote
5 mg USD 90 Get quote
10 mg USD 156 Get quote
50 mg USD 552 Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All Checkpoint Kinase (Chk) Isoform Specific Products:

View All Aurora Kinase Isoform Specific Products:

View All FGFR Isoform Specific Products:

View All CDK Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo[1][2].

IC50 & Target[1]

Chk1

0.49 nM (Ki)

Chk2

47 nM (Ki)

VEGFR2

8 nM (Ki)

Fms

10 nM (IC50)

Yes

14 nM (IC50)

Aurora-A

23 nM (IC50)

FGFR3

23 nM (IC50)

Flt3

25 nM (IC50)

Ret

39 nM (IC50)

CDK1

9.9 μM (Ki)

In Vitro

PF 477736 is a poor inhibitor of CDK1 activity (Ki=9.9 μM, 20,000-fold versus Chk1)[1].
PF 477736 (0.01-1 μM; 16 h) abrogates the camptothecin-induced DNA damage checkpoint in a dose-dependent manner[1].
PF 477736 (10-48 h) abrogates the Gemcitabine-induced S-phase arrest and induces increase in apoptotic cell death in HT29 cells[1].
PF 477736 (180-540 nM; 4-48 h) enhances Gemcitabine cytotoxicity in dose- and time-dependent manner in HT29 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF 477736 (4-60 mg/kg; i.p. for once a day or twice a day for four treatments) potentiates Gemcitabine antitumor activity in Colo205 xenografts[1].
PF 477736 (15 and 30 mg/kg; i.p.) induces histone H3 phosphorylation and DNA damage and increases apoptosis in vivo[1].
PF 477736 (4 mg/kg; i.v.) exhibits low systemic plasma clearance (11.8 mL/min/kg) and terminal half-life (2.9 h) in rats[1].
PF 477736 (4-40 mg/kg; i.p.) exhibits a dose dependent pharmacokinetics[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

419.48

Formula

C₂₂H₂₅N₇O₂

CAS No.

952021-60-2

SMILES

O=C([[email protected]@H](C1CCCCC1)N)NC2=CC3=C(C(C=NNC4=O)=C(N3)C5=CN(N=C5)C)C4=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (297.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3839 mL 11.9195 mL 23.8390 mL
5 mM 0.4768 mL 2.3839 mL 4.7678 mL
10 mM 0.2384 mL 1.1920 mL 2.3839 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.21%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PF 477736PF 00477736PF477736PF-477736PF00477736PF-00477736Checkpoint Kinase (Chk)VEGFRSrcc-FmsAurora KinaseFGFRFLT3RETCDKVascular endothelial growth factor receptorCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RFibroblast growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Cyclin dependent kinaseChk1Chk2GemcitabineantitumorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF 477736
Cat. No.:
HY-10032
Quantity:
MCE Japan Authorized Agent: