Amuvatinib (MP-470)

Amuvatinib (MP-470)は、c-キットとPDGFα(彼らの変異体だけでなく)を含むキナーゼを妨げる、強力でマルチ目標とされたチロシン・キナーゼ阻害剤で、IC50 が 10 nM から31 μMまで。

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Amuvatinib (MP-470) 化学構造
分子量: 447.51



Quality Control & MSDS


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  • 研究分野



製品説明 Amuvatinib (MP-470)は、c-キットとPDGFα(彼らの変異体だけでなく)を含むキナーゼを妨げる、強力でマルチ目標とされたチロシン・キナーゼ阻害剤で、IC50 が 10 nM から31 μMまで。
ターゲット c-KitD816H PDGFRαV561D Flt3D835Y
IC50 10 nM 40 nM 81 nM [1]
In vitro試験 The hydrochloride salt of MP-470 also inhibits several mutants of c-Kit, including c-KitD816V, c-KitD816H, c-KitV560G, and c-KitV654A, as well as a Flt3 mutant (Flt3D835Y) and two PDGFRα mutants (PDGFRαV561D and PDGFRαD842V), with IC50 of 10 nM to 8.4 μM. MP-470 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. [1] MP-470 also inhibits c-Kit and PDGFRα, with IC50 values of 31 μM and 27 μM, respectively. MP-470 demonstrates potent cytotoxicity against MiaPaCa-2, PANC-1, and GIST882 cells, with IC50 of 1.6 μM to 3.0 μM. MP-470 also binds to and inhibits several c-Kit mutants, including c-KitK642E, c-KitD816V, and c-KitK642E/D816V. [2] In MDA-MB-231 cells, MP-470 (1 μM) inhibits tyrosine phosphorylation of AXL. [3] In LNCaP and PC-3, but not DU145 cells, MP-470 exhibits cytotoxicity with IC50 of 4 μM and 8 μM, respectively, and induces apoptosis at 10 μM. In LNCaP cells, MP-470 (10 μM) elicits G1 arrest and decreases phosphorylation of Akt and ERK1/2. [4] In SF767 cells, MP-470 (10 μM) inhibits c-Met phosphorylation and sensitizes cells to radiation. In combination with radiation, MP-470 (10 μM) inhibits glycogen synthase kinase (GSK)3β activity, induces apoptosis, and disrupts the repair of dsDNA breaks probably through suppression of Rad51. [5] [6]
In vivo試験 In mice xenograft models of HT-29, A549, and SB-CL2 cells, MP-470 (10 mg/kg–75 mg/kg via i.p. or 50 mg/kg–200 mg/kg via p.o.) inhibits tumor growth. [1] In mice bearing LNCaP xenograft, MP-470 (20 mg/kg) combined with Erlotinib significantly induces tumor growth inhibition (TGI). [4]
臨床試験 MP-470 is currently under investigation in a Phase II clinical trial for small cell lung carcinoma.

プロトコル (参考用のみ)

キナーゼアッセイ: [2]

Kinase inhibition assay of c-Kit and PDGFRα For the testing of inhibitory activity against c-Kit and PDGFRα, enzymes are incubated with varying concentrations of 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.

細胞アッセイ: [2]

細胞株 MiaPaCa-2, PANC-1, and GIST882 cells
濃度 0–30 μM, dissolved in DMSO
反応時間 96 hours
実験の流れ Cells are plated at a density of 2 × 103 to 1 × 104 cells per well in 100 μL medium on day 0 in 96-well Falcon microtitier plates. On day 1, ten μL of serial dilutions of MP-470 are added to the plates in quadruplicates. After incubation for 4 days, the cells are fixed with 10% Trichloroacetic acid solution. Subsequently, they are labeled with 0.04% Sulforhodamine B (SRB) in 1% acetic acid. After multiple washes to remove the excess dye, 100 μL of 50 mM Tris solution is added to each well in order to dissolve the dye. The absorbance of each well is read on a plate reader at 570 nm. Date are expressed as the percentage of survival of control calculated from the absorbance corrected for background absorbance. The surviving percent of cells is determined by dividing the mean absorbance values of the monoclonal antibody by mean absorbance values of the control and multiplying by 100.

動物実験: [1]

動物モデル Mice (athymic nude) xenograft models of HT-29, A549, and SB-CL2 cells
製剤 Dissolved in corn oil for p.o.; Dissolved in TV-10 (60% propylene glycol, 30% PEG300, 10% water, and 150 mg/mL 2-hydroxypropyl-β-cyclodextrin) or TV-10 (5% ethanol, 40% glycerol, 55% water, and 300 mg/mL cyclodextrin) for i.p.
投薬量 10 mg/kg–75 mg/kg (i.p.) or 50 mg/kg–200 mg/kg (p.o.)
投与方法 Oral gavage (qd5 × 3 weeks) or intraperitoneal injection (qd5 × 2 weeks)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Amuvatinib (MP-470) SDF
分子量 447.51


CAS No. 850879-09-3
保管 2年-20℃
6月-80℃in solvent
別名 HPK 56
溶解度 (25°C) * In vitro DMSO 32 mg/mL (71.5 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-​(1,​3-​benzodioxol-​5-​ylmethyl)​-​4-​benzofuro[3,​2-​d]​pyrimidin-​4-​yl-1-​piperazinecarbothioa​mide

カスタマーフィードバック (4)

Click to enlarge
Source Nat Genet, 2012, 44(8), 852-60. Amuvatinib (MP-470) purchased from Selleck
Method Western blot
Cell Lines ER1, ER2 cells
Concentrations 0-10 uM
Incubation Time 48 h
Results It next sought to validate our genetic findings using pharmacologic inhibitors of AXL. As expected, erlotinib decreased pEGFR, pERK, pAKT, pRelA and increased the levels of cleaved Parp in parental HCC827 cells irrespective of concurrent treatment with MP-470. In contrast, these effects of erlotinib treatment were observed only upon concurrent treatment with MP-470 in the HCC827 ER1 and ER2 cells.

Click to enlarge
Source Oncogene, 2014, 33(10), 1316-24. Amuvatinib (MP-470) purchased from Selleck
Method Western blot
Cell Lines MCF10A cells
Concentrations 0-20 uM
Incubation Time 72 h
Results Immunoblotting of protein expression revealed dose-dependent upregulation of E-Cadherin, β-Catenin and downregulation of N-Cadherin, phospho-AXL, and Snail expression. Since MP470 is known as a c-MET inhibitor we also evaluated the impact of the inhibitor on levels of both c-MET and its activated form phosphorylated at tyrosine 1002. As shown in Figure, c-MET was expressed, albeit weakly in MCF10ATT cells and activation is not detectable.

Click to enlarge
Source Melanoma Res, 2014, 24(5), 448-53. Amuvatinib (MP-470) purchased from Selleck
Method Western blot
Cell Lines WM1366, WM1364 NRAS-mutant melanoma cells
Concentrations 3 uM
Incubation Time 72 h
Results From a mechanistic standpoint, amuvatinib inhibited the phosphorylation of Axl and AKT in the WM1366 and WM1364 NRAS- mutant melanoma cell lines.

Click to enlarge
Source Dr. Yong-Weon Yi from Georgetown University Medical Center. Amuvatinib (MP-470) purchased from Selleck
Method MTT assays
Cell Lines UWB1.289 cells, A2780Cis cells
Concentrations 0-10 μM
Incubation Time 72 h
Results MP-470 treatments reduced UWB1.289 cells and A2780Cis cells growth in a dose-dependent manner.

文献中の引用 (5)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID