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Buparlisib Hydrochloride

产品编号 T16365 CAS 1312445-63-8

别名: NVP-BKM120 Hydrochloride, BKM120 Hydrochloride

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).

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Buparlisib Hydrochloride Chemical Structure

Buparlisib Hydrochloride, CAS 1312445-63-8

规格	价格/CNY	货期
2 mg	￥ 459	5日内发货
5 mg	￥ 772	5日内发货
10 mg	￥ 1,230	5日内发货
1 mL * 10 mM (in DMSO)	￥ 849	5日内发货

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Buparlisib Hydrochloride 的其他形式现货产品:

Buparlisib

其他形式的 Buparlisib Hydrochloride:

Buparlisib
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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).
靶点活性	mTOR:4.6 μM, p110α-E545K:99 nM, p110α:52 nM, p110γ:262 nM, p110δ:116 nM, p110α-H1047R:58 nM, p110β:166 nM, VPS34:2.4 μM
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].

别名	NVP-BKM120 Hydrochloride, BKM120 Hydrochloride
分子量	446.85
分子式	C18H22ClF3N6O2
CAS No.	1312445-63-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (111.89 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2379 mL	11.1894 mL	22.3789 mL	55.9472 mL
	5 mM	0.4476 mL	2.2379 mL	4.4758 mL	11.1894 mL
	10 mM	0.2238 mL	1.1189 mL	2.2379 mL	5.5947 mL
	20 mM	0.1119 mL	0.5595 mL	1.1189 mL	2.7974 mL
	50 mM	0.0448 mL	0.2238 mL	0.4476 mL	1.1189 mL
	100 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5595 mL

计算器

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参考文献

1. Burger MT, et al. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett. 2011 Aug 26;2(10):774-9. 2. Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone. J Mol Med (Berl). 2012 Jun;90(6):695-706.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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