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

PF 477736  (Synonyms: PF 00477736)

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

Molarity Calculator

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 Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 90 In-stock
10 mg USD 156 In-stock
50 mg USD 552 In-stock
100 mg   Get quote  
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Customer Review

Based on 5 publication(s) in Google Scholar

PF 477736 Related Antibodies

Top Publications Citing Use of Products

View All Checkpoint Kinase (Chk) Isoform Specific Products:

View All Isoforms
Chk1 Chk2

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All Src Isoform Specific Products:

View All Isoforms
Lck Fyn Blk

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

View All FGFR Isoform Specific Products:

View All Isoforms
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 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) dose-dependently abrogates the camptothecin-induced DNA damage checkpoint in CA46 cells[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].

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

PF 477736 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C([C@@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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.21%

SDS (393 KB)

COA (254 KB) LCMS (113 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3839 mL 11.9195 mL 23.8390 mL 59.5976 mL
5 mM 0.4768 mL 2.3839 mL 4.7678 mL 11.9195 mL
10 mM 0.2384 mL 1.1920 mL 2.3839 mL 5.9598 mL
15 mM 0.1589 mL 0.7946 mL 1.5893 mL 3.9732 mL
20 mM 0.1192 mL 0.5960 mL 1.1920 mL 2.9799 mL
25 mM 0.0954 mL 0.4768 mL 0.9536 mL 2.3839 mL
30 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9866 mL
40 mM 0.0596 mL 0.2980 mL 0.5960 mL 1.4899 mL
50 mM 0.0477 mL 0.2384 mL 0.4768 mL 1.1920 mL
60 mM 0.0397 mL 0.1987 mL 0.3973 mL 0.9933 mL
80 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7450 mL
100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5960 mL
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PF 477736 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF 477736952021-60-2PF 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

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