Amuvatinib (MP-470)

製品コードS1244 別名:HPK 56

Amuvatinib (MP-470)化学構造

分子量(MW):447.51

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。

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

カスタマーフィードバック(4)

  • Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers. Data represent 3 independent experiments.

    Nat Genet 2012 44(8), 852-60. Amuvatinib (MP-470) purchased from Selleck.

    Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.

    Oncogene 2014 33(10), 1316-24. Amuvatinib (MP-470) purchased from Selleck.

  • Amuvatinib (3 umol/l, 72 h) leads to decreased pAXL, pAKT, and pERK expression by western blot.

    Melanoma Res 2014 24(5), 448-53. Amuvatinib (MP-470) purchased from Selleck.

    For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of MP-470 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. Amuvatinib (MP-470) purchased from Selleck.

製品安全説明書

c-Kit阻害剤の選択性比較

生物活性

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-Kit (D816H) [1] PDGFRα (V561D) [1] FLT3 (D835Y) [1]
10 nM 40 nM 81 nM
体外試験

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]

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[2]
+ 展開

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.
細胞試験: [2]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 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)
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 32 mg/mL (71.5 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 447.51
化学式

C23H21N5O3S

CAS No. 850879-09-3
保管
in solvent
別名 HPK 56

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01357395 Unknown status Small Cell Lung Carcinoma Astex Pharmaceuticals May 2011 Phase 2
NCT00881166 Completed Malignant Disease Astex Pharmaceuticals November 2007 Phase 1
NCT00894894 Completed Solid Tumors Astex Pharmaceuticals May 2007 Phase 1
NCT00504205 Terminated Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific Astex Pharmaceuticals|National Cancer Institute (NCI) May 2007 --

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

c-Kit信号経路図

c-Kit Inhibitors with Unique Features

相関c-Kit製品

Tags: Amuvatinib (MP-470)を買う | Amuvatinib (MP-470) ic50 | 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)化学構造 | Amuvatinib (MP-470)分子量 | Amuvatinib (MP-470)代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID