化合物 Amuvatinib hydrochloride,Amuvatinib hydrochloride

化合物 Amuvatinib hydrochloride|T14282|TargetMol

價(jià)格	詢(xún)價(jià)
包裝	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2025-07-23

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產(chǎn)品詳情

中文名稱(chēng):化合物 Amuvatinib hydrochloride	英文名稱(chēng):Amuvatinib hydrochloride
CAS:1055986-67-8	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T14282

Product Introduction

Bioactivity

名稱(chēng)	Amuvatinib hydrochloride
描述	Amuvatinib hydrochloride (MP470 hydrochloride) is an orally administred multi-targeted tyrosine kinase inhibitor that exhibits strong efficacy against mutant forms of c-Kit, PDGFRα, Flt3, c-Met, and c-Ret, while also acting as a suppressor of DNA repair by inhibiting the RAD51 protein, which is crucial for repairing DNA damage[1][2][3]. This dual mechanism contributes to its antineoplastic activity[4].
體外活性	Amuvatinib (MP470), a novel receptor tyrosine kinase (RTK) inhibitor has shown growth inhibitory activity against a variety of cancer cell lines. Amuvatinib (MP470) inhibits c-Kit (D816V), c-Kit (D816H), c-Kit (V560G), c-Kit (V654A), PDGFRα (D842V), and PDGFRα (V561D) with IC50s of 950 nM, 10 nM, 34 nM, 127 nM, 81 nM, and 40 nM, respectively[4]. Amuvatinib (0.1-10 μM, 4 days incubation) is effective on LNCaP and PC-3 cells with IC50s of ~4 μM and 8 μM, respectively. When Erlotinib (10 μM) is combined with varying doses of Amuvatinib, the IC50 of Amuvatinib decreases to 2 μM on LNCaP cells[5]. Akt activity (as measured by phosphorylation on Ser473) is significantly reduced by 10 μM Amuvatinib (treated for 30 hours) alone. However it is not reduced by Erlotinib or Imatinib Mesylate (IM). Amuvatinib plus Erlotinib completely abolished Akt phosphorylation in LNCaP cells with an unchanged total protein level of Akt[5].
體內(nèi)活性	Four LNCaP xenograft arms each with 12 mice are dosed intraperitoneally with DMSO (control) or Erlotinib 80 mg/kg or Amuvatinib (MP470) 50 mg/kg or Erlotinib 80 mg/kg plus Amuvatinib 50 mg/kg daily for 2 weeks and then observed for a further 11 days. TGI in the group receiving 10 mg/kg Amuvatinib+80 mg/kg Erlotinib is not significantly different from the control group. However, mice receiving 20 mg/kg Amuvatinib+80 mg/kg Erlotinib have a significant TGI compared to the control group (p=0.01)[5]. Individual therapy with Amuvatinib or Erlotinib shows modest tumor growth inhibition (TGI), while Amuvatinib plus Erlotinib has a marked effect on TGI (45-65%). But, due to the high doses of Amuvatinib used, only five or one mouse remained alive in the combination arm at the end of treatment or at the end of the study, respectively. Therefore the Amuvatinib dose is reduced to 10 mg/kg or 20 mg/kg for the combination treatment.
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
關(guān)鍵字	PDGFRαV561D \| PDGFRαD842V \| MP-470 Hydrochloride \| MP470 Hydrochloride \| MP 470 Hydrochloride \| HPK-56 Hydrochloride \| HPK56 Hydrochloride \| HPK 56 Hydrochloride \| c-KitV654A \| c-KitV560G \| c-KitD816V \| c-KitD816H \| Amuvatinib Hydrochloride \| Amuvatinib hydrochloride

關(guān)鍵字： MP470 hydrochloride|||HPK 56 hydrochloride|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶(hù)群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿(mǎn)足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿(mǎn)足客戶(hù)的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專(zhuān)業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （13年）	注冊(cè)資本	589.8595萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù)	經(jīng)營(yíng)模式	貿(mào)易,工廠(chǎng),試劑,定制,服務(wù)

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公司成立：13年
注冊(cè)資本：589.8595萬(wàn)人民幣
企業(yè)類(lèi)型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：抑制劑&激動(dòng)劑，天然產(chǎn)物，重組蛋白，化合物庫(kù)，技術(shù)服務(wù)
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