Amuvatinib (MP-470)

Amuvatinib (MP-470)は一種の有効で、c-Kit、PDGFαとFlt3に作用する多ターゲット阻害剤で、IC50値が10 nM、40 nMと81 nMにそれぞれ分かれることです。臨床2期。

価格 在庫  
USD 151 あり
USD 264 あり
USD 296 あり
USD 466 あり
USD 1096 あり

Amuvatinib (MP-470) 化学構造
分子量: 447.51





  • Compare c-Kit Inhibitors
  • 研究分野



製品説明 Amuvatinib (MP-470)は一種の有効で、c-Kit、PDGFαとFlt3に作用する多ターゲット阻害剤で、IC50値が10 nM、40 nMと81 nMにそれぞれ分かれることです。臨床2期。
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 3年-20℃
2年-80℃in solvent
別名 HPK 56
溶解度 (25°C) * In vitro DMSO 32 mg/mL (71.5 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

文献中の引用 (5)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related c-Kit 阻害剤

  • Erlotinib

    Erlotinibは一種のEGFR阻害剤で、このIC50値が2 nMです。Erlotinibは、EGFRに対する敏感性は人間c-Src或いはv-Abに対する敏感性より1000倍以上が高くなります。

  • R428 (BGB324)

    R428 (BGB324)は一種のAxl阻害剤で、IC50値が14 nMです。R428 (BGB324)は、Axlに作用する選択性はAblに作用する選択性より100倍以上が高くなって、MerとTyro3に作用する選択性より50倍-100倍が高くなって、InsR、EGFR、HER2とPDGFRβに作用する選択性より100倍余りが高くなります。

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397)は一種の経口有効な多ターゲットCSF-1R、KitとFlt3受容体チロシンキナーゼ阻害剤で、IC50値が20 nM、10 nMと160 nMにそれぞれ分かれることです。臨床3期。

  • PF-06463922

    PF-06463922は一種の有効な二重ALK/ ROS1阻害剤で、ROS1、ALK (WT)とALK (L1196M)に作用する時のKi値が0.02 nM以下、0.07 nM以下、0.7 nMにそれぞれ分かれることです。臨床1期。

  • Masitinib (AB1010)

    Masitinib (AB1010)は一種の新たなKitとPDGFRα/β阻害剤で、IC50値が200 nMと540 nM/800 nMに分かれることです。Masitinib (AB1010)はABLとc-Fmsを抑制する効果が少し弱いです。臨床3期。

    Features:Potential low side-effect profile.

  • OSI-930

    OSI-930は一種の有効なKit、KDRとCSF-1R阻害剤で、IC50値が80 nM、9 nMと15 nMにそれぞれ分かれることです。OSI-930はFlt-1、c-RafとLckに対して、適度な抑制活性がありますが、PDGFRα/β、Flt-3とAblを抑制する活性が少し弱いです。臨床1期。

  • Gefitinib (ZD1839)

    Gefitinib (ZD-1839)は一種のEGFR阻害剤で、NR6wtEGFRとNR6Wの細胞中のTyr1173、Tyr992、Tyr1173とTyr992に作用する時のIC50値が37 nM、37nM、26 nMと57 nMにそれぞれ分かれることです。

    Features:A potent EGFR tyrosine kinase inhibitor.

  • Erlotinib HCl (OSI-744)

    Erlotinib HCl (OSI-744)は一種のEGFR阻害剤で、無細胞試験で、IC50値が2 nMです。Erlotinib HCl (OSI-744)はEGFRに作用する選択性は人間c-Src或いはv-Ablに作用する選択性より1000倍以上が高くなります。

  • Crizotinib (PF-02341066)

    Crizotinib (PF-02341066)は一種の有効なc-MetとALK阻害剤で、細胞試験でIC50値が11 nMと24 nMです。


Tags: Amuvatinib (MP-470)を買う | Amuvatinib (MP-470)供給者 | Amuvatinib (MP-470)を購入する | Amuvatinib (MP-470)費用 | Amuvatinib (MP-470)生産者 | オーダーAmuvatinib (MP-470) | Amuvatinib (MP-470)代理店
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID