Pulrodemstat|T39258|TargetMol

價(jià)格	￥10600
包裝	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:Pulrodemstat	英文名稱:Pulrodemstat
CAS:1821307-10-1	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.
產(chǎn)品類別: 抑制劑
貨號(hào): T39258

Product Introduction

Bioactivity

Name	Pulrodemstat
Description	Pulrodemstat (CC-90011) is a highly potent and selective inhibitor of lysine specific demethylase-1 (LSD1). It exhibits a reversible mode of action and can be administered orally. With an impressive IC50 of 0.25 nM, Pulrodemstat effectively suppresses the enzymatic activity of LSD1. Notably, it demonstrates minimal inhibition against LSD2, MOA-A, and MAO-B enzymes. Moreover, Pulrodemstat possesses remarkable anticancer properties, promoting differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells.
In vitro	Pulrodemstat (CC-90011, Compound 11) shows potent induction of on-target cellular differentiation marker CD11b in THP-1 cell line with an EC 50 of 7 nM, antiproliferative activity in AML kasumi-1 cells with an EC 50 of 2 nM[1]. Suppression of GRP is observed with treatment of Pulrodemstat (4 days) in a dose-dependent manner and at pharmacologically useful concentrations (EC 50 =3 nM, H209 and 4 nM, H1417). Pulrodemstat (12 days) treatment of SCLC cells results in potent antiproliferative activity (EC 50 =6 nM, H1417) that correlated with GRP suppression[1].
In vivo	Pulrodemstat (CC-90011; 5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1]. Pulrodemstat (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1]. After i.v. administration, Pulrodemstat (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. Pulrodemstat (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC 0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1]. Animal Model: BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1]Dosage: 5 mg/kg Administration: Oral administration; daily; for 30 days Result: Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss.
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Keywords	CC90011 \| Pulrodemstat \| CC 90011

關(guān)鍵字： LSD1-IN-7|||CC-90011|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(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多種滿足不同需求的化合物庫(kù)，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(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)	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(yíng)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(wàn)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(yíng)產(chǎn)品：小分子抑制劑、藥物篩選化合物庫(kù)、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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