化合物 Buparlisib Hydrochloride|T16365|TargetMol

Buparlisib Hydrochloride
1312445-63-8

￥1230 10mg 起订

￥459 2mg 起订

￥772 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 Buparlisib Hydrochloride

英文名称：: Buparlisib Hydrochloride

CAS号：: 1312445-63-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

产品类别：: 抑制剂

货号：: T16365

Product Introduction

Bioactivity

名称	Buparlisib Hydrochloride
描述	Buparlisib Hydrochloride is an inhibitor of pan-class I PI3K (IC50: 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively).
体外活性	NVP-BKM120 shows lower potency against class III and class IV PI3K's, where 2, 5, >5, and >25 μM biochemical activity is observed for inhibition of VPS34, mTOR, DNAPK, and PI4K, respectively. Buparlisib causes multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. Buparlisib has 50-300 nM activity for class I PI3K's, including the most common p110α mutants. Buparlisib ( ≥10 μM) induces significant apoptosis in all tested MM cell lines at 24 h (P<0.05, compares with control). Buparlisib (10 μM; 24-h) treatment is chosen in the following experiments if not stated otherwise. Buparlisib treatment causes dose-dependent growth inhibition in all tested MM cell lines. Buparlisib IC50 varies among tested MM cells. At 24 h treatment, IC50 for ARP-1, ARK, and MM.1R is between 1 and 10 μM, while IC50 for MM.1S is <1 μM, and IC50 for U266 is between 10 and 100 μM. Buparlisib treatment results in MM cell growth inhibition and apoptosis in a dose- and time-dependent manners[1][2].
体内活性	Buparlisib (p.o.; 3, 10, 30, 60, and 100 mg/kg) results in a dose-dependent modulation of pAKTSer473, in A2780 xenograft tumors. Mice receiving Buparlisib (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compared with control mice, which are measured as tumor volume (P<0.05) and level of circulating human kappa chain (P<0.05). Buparlisib treatment significantly prolongs the survival of tumor-bearing mice (P<0.05). Partial inhibition of pAKTSer473 is observed at 3 and 10 mg/kg, and near-complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma and tumor drug exposure[1][2].
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (111.89 mM)
关键字	BKM 120 Hydrochloride \| NVP-BKM-120 Hydrochloride \| NVP-BKM 120 Hydrochloride \| BKM-120 Hydrochloride \| Buparlisib Hydrochloride

NVP-BKM120 Hydrochloride|||BKM120 Hydrochloride|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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