PLX647 dihydrochloride,PLX647 dihydrochloride

PLX647 dihydrochloride|T39194|TargetMol

價(jià)格	￥10600
包裝	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-30

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產(chǎn)品詳情

中文名稱:PLX647 dihydrochloride	英文名稱:PLX647 dihydrochloride
CAS:1779796-38-1	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
產(chǎn)品類別: 抑制劑
貨號(hào): T39194

Product Introduction

Bioactivity

名稱	PLX647 dihydrochloride
描述	PLX647 dihydrochloride is a potent and selective dual inhibitor of FMS and KIT kinases, with IC50 values of 28 nM and 16 nM, respectively. At a concentration of 1 μM, PLX647 dihydrochloride demonstrates superior selectivity against a wide range of 400 kinases, except FLT3 and KDR, where IC50 values are 91 nM and 130 nM, respectively. This orally active compound holds great potential for targeted kinase inhibition.
體外活性	In vitro, PLX647 dihydrochloride potently inhibits proliferation of BCR-FMS cells, with an IC 50 of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647 dihydrochloride, with an IC 50 of 180 nM. PLX647 dihydrochloride also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC 50 =380 nM) and M-07e (IC 50 =230 nM), which express FMS and KIT, respectively[1]. PLX647 dihydrochloride potently inhibits the growth of FLT3-ITD-expressing MV4-11 cells (IC 50 =110 nM). PLX647 dihydrochloride displays minimal inhibition of the proliferation of Ba/F3 cells expressing BCR-KDR (IC 50 =5 μM). PLX647 dihydrochloride inhibits osteoclast differentiation with an IC 50 of 0.17 μM[1].
體內(nèi)活性	PLX647 dihydrochloride (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes[1]. PLX647 dihydrochloride (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release[1]. PLX647 dihydrochloride (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis[1]. PLX647 dihydrochloride (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 dihydrochloride (30 mg/kg BID) is able to prevent bone damage by the tumor cells[1]. Animal Model: Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]Dosage: 40 mg/kg Administration: P.o.; twice daily for 7 days Result: Resulted in reduction in the levels of F4/80+ macrophages by 77%. Animal Model: 7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)[1]Dosage: 20 mg/kg, 80 mg/kg Administration: P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days Result: 20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
關(guān)鍵字	PLX-647 Dihydrochloride \| PLX647 \| PLX647 dihydrochloride \| PLX 647 \| PLX-647 \| PLX647 Dihydrochloride \| PLX-647 dihydrochloride \| PLX 647 Dihydrochloride

關(guān)鍵字： PLX647 dihydrochloride|TargetMol

公司簡介

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)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(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，全方位滿足客戶的定制需求。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 （12年）	注冊(cè)資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場(chǎng)三路238號(hào)8樓

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