PF-477736 (PF-00477736)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1380 | Check With Us |
| 500mg | $2150 | Check With Us |
| 1g | $3225 | Check With Us |
: Cat #: V1586 CAS #: 952021-60-2 Purity ≥ 98%
Description: PF-477736 (also known as PF-736; PF-00477736; PF477736) is a novel, selective, potent and ATP-competitive Chk1 inhibitor with potential antitumor activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 419.48 |
|---|---|
| Molecular Formula | C22H25N7O2 |
| CAS No. | 952021-60-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 6 mg/mL (14.3 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 2% DMSO+40% PEG 300: 5 mg/mL |
| Synonyms | PF-736,PF-00477736; PF-477736; PF-00477736; PF 477736; PF 00477736; PF00477736; PF477736 |
| Protocol | In Vitro | PF-00477736 was identified as a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a K(i) of 0.49 nM. PF-00477736 abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin. |
|---|---|---|
| In Vivo | To test the efficacy of PF-477736 in vivo, this study inoculated NOD/SCID mice with A549 isogenic lines subcutaneously and treated with PF-477736 twice on indicated days. LIMD1+/+ tumours were unaffected by PF-477736 treatment in vivo, however this study observed a significant decrease in tumour growth in the LIMD1−/− tumours upon treatment (Figs. 4E and S4A, B). Staining of these tumours with markers for cell proliferation (Ki67, Figs. 4F and S4C) and apoptosis (cleaved caspase-3, Figs. 4G and S4D), revealed that PF-477736 selectivity inhibits proliferation in LIMD1-deficient lung xenografts and increases apoptosis within these tumours, in agreement with in vitro data. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3839 mL | 11.9195 mL | 23.8390 mL | 47.6781 mL |
| 5mM | 0.4768 mL | 2.3839 mL | 4.7678 mL | 9.5356 mL |
| 10mM | 0.2384 mL | 1.1920 mL | 2.3839 mL | 4.7678 mL |
| 20mM | 0.1192 mL | 0.5960 mL | 1.1920 mL | 2.3839 mL |
| Quality Control Documentation |
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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: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.