Name: Amuvatinib (MP-470)
Brand: Selleck Chemicals
SKU: S1244
Availability: InStock
Rating: 5 (21 reviews)

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other c-Kit Inhibitors	Masitinib Sitravatinib (MGCD516) OSI-930 PDGFR inhibitor 1 ISCK03 Elenestinib phosphate M4205（IDRX-42） Masitinib mesylate AZD3229 Bezuclastinib

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
GIST	Function assay			Inhibition of AXL in human GIST cells, IC50<1μM	26555154
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Caco-2	Function assay		48 hrs	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=0.02μM	ChEMBL
Caco-2	Function assay		48 hrs	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=0.06μM	ChEMBL
GIST882	Function assay		4 days	Inhibition of c-kit gain of function mutant in human GIST882 cells measured after 4 days by sulforhodamine B assay, IC50=1.6μM	ChEMBL
GIST882	Function assay		96 hrs	Inhibition of c-kit gain of function mutant in human GIST882 cells after 96 hrs by Cell-Titer Glo luciferase assay, IC50=1.6μM	ChEMBL
MIAPaCa2	Function assay		4 days	Inhibition of PDGFRA in human MIAPaCa2 cells measured after 4 days by sulforhodamine B assay, IC50=2.1μM	ChEMBL
PANC1	Function assay		4 days	Inhibition of PDGFRA in human PANC1 cells measured after 4 days by sulforhodamine B assay, IC50=3μM	ChEMBL
SF-767	Cytotoxicity assay	1 uM	24 hrs	Cytotoxicity against human SF-767 cells assessed as cell death at 1 uM after 24 hrs by MTS assay	ChEMBL
SF-767	Cytotoxicity assay	1 uM	24 hrs	Cytotoxicity against human SF-767 cells assessed as cell death at 1 uM in presence of 800Gy ionizing radiation after 24 hrs by MTS assay	ChEMBL
SBcl2	Antitumor assay		5 days	Antitumor activity against human SBcl2 cells xenografted in ip dosed athymic nude mouse assessed as reduction in tumor growth administered as qd for 5 days	ChEMBL
HT-29	Function assay			Suppression of ionizing radiation-induced Rad51 expression in human HT-29 cells pretreated with compound followed by ionizing radiation by Western blot analysis	ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 32 mg/mL (71.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (10.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	447.51	Formula	C₂₃H₂₁N₅O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	850879-09-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HPK 56			Smiles	C1CN(CCN1C2=NC=NC3=C2OC4=CC=CC=C43)C(=S)NCC5=CC6=C(C=C5)OCO6

Mechanism of Action

Targets/IC₅₀/Ki	c-Met RAD51 c-RET c-Kit (D816H) 10 nM PDGFRα (V561D) 40 nM FLT3 (D835Y) 81 nM
In vitro	The hydrochloride salt of Amuvatinib (MP-470) inhibits several mutants of c-Kit, including c-Kit^D816V, c-Kit^D816H, c-Kit^V560G, and c-Kit^V654A, as well as a Flt3 mutant (Flt3^D835Y) and two PDGFRα mutants (PDGFRα^V561D and PDGFRα^D842V), with IC50 of 10 nM to 8.4 μM. It also binds to and inhibits several c-Kit mutants, including c-Kit^K642E, c-Kit^D816V, and c-Kit^K642E/D816V. This compound potently inhibits the proliferation of OVCAR-3, A549, NCI-H647, DMS-153, and DMS-114 cells, with IC50 of 0.9 μM–7.86 μM. It also inhibits c-Kit and PDGFRα, with IC50 values of 31 μM and 27 μM, respectively. It demonstrates potent cytotoxicity against MiaPaCa-2, PANC-1, and GIST882 cells, with IC50 of 1.6 μM to 3.0 μM. In MDA-MB-231 cells, it (1 μM) inhibits tyrosine phosphorylation of AXL. In LNCaP and PC-3, but not DU145 cells, it exhibits cytotoxicity with IC50 of 4 μM and 8 μM, respectively, and induces apoptosis at 10 μM. In LNCaP cells, it (10 μM) elicits G1 arrest and decreases phosphorylation of Akt and ERK1/2. In SF767 cells, it (10 μM) inhibits c-Met phosphorylation and sensitizes cells to radiation. In combination with radiation, it (10 μM) inhibits glycogen synthase kinase (GSK)3β activity, induces apoptosis, and disrupts the repair of dsDNA breaks probably through suppression of Rad51.
Kinase Assay	Kinase inhibition assay of c-Kit and PDGFRα
Kinase Assay	For the testing of inhibitory activity against c-Kit and PDGFRα, enzymes are incubated with varying concentrations of Amuvatinib (MP-470) and radiolabeled γ-³²P-ATP. After 30 min, the reaction mixtures are electrophoresed on an acrylamide gel and autophosphorylation, quantitated by the amount of radioactivity incorporated into the enzyme, is assayed.
In vivo	In mice xenograft models of HT-29, A549, and SB-CL2 cells, Amuvatinib (MP-470) (10 mg/kg–75 mg/kg via i.p. or 50 mg/kg–200 mg/kg via p.o.) inhibits tumor growth. In mice bearing LNCaP xenograft, this compound (20 mg/kg) combined with Erlotinib significantly induces tumor growth inhibition (TGI).
References	[1] http://www.patentstorm.us/patents/7820684.html [2] http://www.wipo.int/patentscope/search/en/WO2005037825 [3] https://pubmed.ncbi.nlm.nih.gov/17325667/ [4] https://pubmed.ncbi.nlm.nih.gov/19432987/ [5] https://pubmed.ncbi.nlm.nih.gov/20028557/ [6] https://pubmed.ncbi.nlm.nih.gov/21903282/ [7] https://pubmed.ncbi.nlm.nih.gov/20563581/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		24950457
Western blot	p-AXL / AXL / p-AKT / AKT / ERK / Rad51		24950457

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01357395	Completed	Small Cell Lung Carcinoma	Astex Pharmaceuticals Inc.	May 2011	Phase 2

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Amuvatinib (MP-470) c-Kit inhibitor

Chemical Structure

Molecular Weight: 447.51