PHA-665752
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 | $750 | Check With Us |
| 500mg | $1150 | Check With Us |
| 1g | $1725 | Check With Us |
: Cat #: V0591 CAS #: 477575-56-7 Purity ≥ 98%
Description: PHA-665752 (PHA665752) is a novel, potent, selective and ATP-competitive small molecule inhibitor of c-Met Kinase with potential antitumor activity.
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| Molecular Weight (MW) | 641.61 |
|---|---|
| Molecular Formula | C32H34Cl2N4O4S |
| CAS No. | 477575-56-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 128 mg/mL (199.5 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 2% DMSO+castor oil: 5 mg/mL |
| SMILES Code | O=C1NC2=C(C=C(S(=O)(CC3=C(Cl)C=CC=C3Cl)=O)C=C2)/C1=C/C4=C(C)C(C(N5[C@@H](CN6CCCC6)CCC5)=O)=C(C)N4 |
| Synonyms | PHA-665752; PHA665752; PHA 665752 |
| Protocol | In Vitro | PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells. PHA-665752 (0-1.25 μM; 72 hours) induces apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells. PHA-665752 (0-1.25 μM; 18 hours) potently inhibits HGF and c-Met-driven phenotypes such as cell growth (proliferation and survival), cell motility, invasion, and/or morphology of a variety of tumor cells. PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines. PHA-665752 shows potent inhibition of c-Met RTK autophosphorylation in NIH3T3 cells engineered to express high levels of c-Met and hepatocyte growth factor (HGF). PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated. PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a Ki of 4 nM and an IC50 of 9 nM. |
|---|---|---|
| In Vivo | PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model. PHA-665752 (7.5-30 mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30 mg/kg/day, 15 mg/kg/day, and 7.5 mg/kg/day doses, respectively. |
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 | 1.5586 mL | 7.7929 mL | 15.5858 mL | 31.1716 mL |
| 5mM | 0.3117 mL | 1.5586 mL | 3.1172 mL | 6.2343 mL |
| 10mM | 0.1559 mL | 0.7793 mL | 1.5586 mL | 3.1172 mL |
| 20mM | 0.0779 mL | 0.3896 mL | 0.7793 mL | 1.5586 mL |
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
Note:
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