PHA-665752

Name: PHA-665752
Brand: MedChemExpress
SKU: HY-11107
Rating: 5.0 (14 reviews)

Cat. No.: HY-11107 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (K_i=4 nM; IC₅₀=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity.

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

PHA-665752 Chemical Structure

CAS No. : 477575-56-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 106	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 106	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 365	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of PHA-665752:

PHA-665752-d8 hydrate Get quote

11 Publications Citing Use of MCE PHA-665752

: PHA-665752 purchased from MedChemExpress. Usage Cited in: Am J Transl Res. 2023 Feb 28;15(2):896-913.; PHA-665752 significantly decreases the migration rate at 24 h and 48 h in Huh-7^R cells.

: PHA-665752 purchased from MedChemExpress. Usage Cited in: Respir Res. 2020 Aug 14;21(1):215. [Abstract]; Immunoblotting reveals that c-Met in the plasma membrane is phosphorylated in response to the binding of HGF, and this c-Met phosphorylation is abolished by PHA-665752 in the LPS-transfected endothelial cells.

: PHA-665752 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 13;8(24):38717-38730. [Abstract]; KU812/IR cells are exposed to the indicated concentrations of Imatinib or PHA665752. After incubation for 48 h, the cytoplasmic fractions are extracted and then subjected to SDS-PAGE/immunoblotting with anti-phospho-MET, anti-phospho-ABL1, anti-phospho-ERK1/2, anti-phospho-AKT, anti-phospho-JNK, anti-MET, anti-ABL1, anti-ERK1/2, anti-AKT, and anti-JNK antibodies. Anti-β-ACTIN antibody is used as internal standards.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Ki: 4 nM^[1]
IC50: 9 nM (c-Met)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	9 nM Compound: 3, PHA-665752	Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method	[PMID: 21812414]
HCC827	IC₅₀	15.7 μM Compound: PHA-665752	Cytotoxicity against erlotinib-sensitive human HCC827A cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against erlotinib-sensitive human HCC827A cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27563407]
HCC827	IC₅₀	8.9 μM Compound: PHA-665752	Cytotoxicity against erlotinib-resistant human HCC827B cells expressing MET assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against erlotinib-resistant human HCC827B cells expressing MET assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27563407]
TAMH	IC₅₀	8.9 μM Compound: PHA-665752	Cytotoxicity against TAMH assessed as reduction in cell viability after 24 hrs by cell titer glo based luminescence assay Cytotoxicity against TAMH assessed as reduction in cell viability after 24 hrs by cell titer glo based luminescence assay	[PMID: 27563407]

In Vitro

PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a K_i of 4 nM and an IC₅₀ of 9 nM^[1].
PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated^[1].
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)^[1].
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^[1].
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^[1].
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^[1].
PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	S114 cells, GTL-16 cells, NCI-H441 cells, or BxPC-3 cells
Concentration:	0 μM, 0.002 μM, 0.01 μM, 0.05 μM, 0.25 μM, 1.25 μM
Incubation Time:	18 hours
Result:	Potently inhibited HGF and c-Met-driven cell growth.

Apoptosis Analysis^[1]

Cell Line:	GTL-16 cells
Concentration:	0 μM, 0.002 μM, 0.01 μM, 0.05 μM, 0.25 μM, 1.25 μM
Incubation Time:	72 hours
Result:	Induced apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells. Immunoblot Analysis.

Western Blot Analysis^[1]

Cell Line:	A549 cells
Concentration:	0.0125 μM, 0.025 μM,0.05 μM,0.1 μM,0.2 μM
Incubation Time:	4 hours
Result:	Potent inhibited HGF-induced c-Met phosphorylation in A549 cells.

In Vivo

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^[1].
PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model^[1].

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

Animal Model:	Female athymic mice (nu/nu, 8–12 weeks) bearing S114 or GTL-16 tumor xenografts^[1]
Dosage:	7.5 mg/kg/day, 15 mg/kg/day, 30 mg/kg/day
Administration:	Intravenous injection; for 9 days
Result:	Demonstrated statistically significant dose-dependent tumor growth inhibition.

Molecular Weight

641.61

Formula

C₃₂H₃₄Cl₂N₄O₄S

CAS No.

477575-56-7

Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)S(=O)(CC4=C(C=CC=C4Cl)Cl)=O)=O)=C1C)C)N5[C@H](CCC5)CN6CCCC6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (38.96 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	1.5586 mL	7.7929 mL	15.5858 mL
5 mM	0.3117 mL	1.5586 mL	3.1172 mL
10 mM	0.1559 mL	0.7793 mL	1.5586 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.5 mg/mL (3.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (3.90 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.86%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (252 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Christensen JG, et al. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003 Nov 1;63(21):7345-55. [Content Brief]

[2]. Ma PC. et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res. 2005 Mar 15;11(6):2312-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5586 mL	7.7929 mL	15.5858 mL	38.9645 mL
	5 mM	0.3117 mL	1.5586 mL	3.1172 mL	7.7929 mL
	10 mM	0.1559 mL	0.7793 mL	1.5586 mL	3.8964 mL
	15 mM	0.1039 mL	0.5195 mL	1.0391 mL	2.5976 mL
	20 mM	0.0779 mL	0.3896 mL	0.7793 mL	1.9482 mL
	25 mM	0.0623 mL	0.3117 mL	0.6234 mL	1.5586 mL
	30 mM	0.0520 mL	0.2598 mL	0.5195 mL	1.2988 mL

PHA-665752 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:

PHA-665752477575-56-7PHA665752PHA 665752c-Met/HGFRAutophagyApoptosisInhibitorinhibitorinhibit

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PHA-665752

Customer Review

Other Forms of PHA-665752:

PHA-665752 Related Antibodies

11 Publications Citing Use of MCE PHA-665752

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•Related Screening Libraries:

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References

Customer Review

PHA-665752 Related Antibodies

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Complete Stock Solution Preparation Table

PHA-665752 Related Classifications

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