| 中文名称： | 布帕x西盐酸盐 | 中文别名： | 布帕x西盐酸盐 |
|---|---|---|---|
| 英文名称： | Buparlisib Hydrochloride | CAS： | 1312445-63-8 |
| 产品分类： | 小分子化合物 | 纯度： | ≥98% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| IB2070 | 索莱宝 | ≥98% | 5mg | 有现货 | 760.00 元 |
| IB2070 | 索莱宝 | ≥98% | 10mg | 有现货 | 1,190.00 元 |
| IB2070 | 索莱宝 | ≥98% | 50mg | 有现货 | 2,290.00 元 |
| IB2070 | 索莱宝 | ≥98% | 100mg | 有现货 | 3,790.00 元 |
| 标准名称: | BKM120(盐酸盐) | 英文名称： | Buparlisib Hydrochloride |
|---|---|---|---|
| CAS： | 1312445-63-8 | 分子式： | C18H22ClF3N6O2 |
| 分子量： | 446.854492664337 | 颜色与性状： | |
| 密度： | 沸点： | ||
| 熔点： | 水溶性： |
| CAS | 1312445-63-8 |
| 中文名称 | 布帕x西盐酸盐 |
| 英文名称 | Buparlisib Hydrochloride |
| 别名 | ;BKM120-AAA;UNII-194LK4P5K1; |
| 分子式 | C18H22ClF3N6O2 |
| 分子量 | 446.85 |
| 规格 | 5mg ; 10mg ; 50mg ; 100mg |
| 溶解性 | Soluble in DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| SMILES | C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4.Cl |
| InChIKey | DGPLYAXBXJXEID-UHFFFAOYSA-N |
| InChI | InChI=1S/C18H21F3N6O2.ClH/c19-18(20，21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27;/h9-11H，1-8H2，(H2，22，23);1H |
| PubChem CID | 66577015 |
| 靶点 | PI3K |
| 通路 | PI3K/Akt/mTOR |
| 背景说明 | 是一种 pan-class I PI3K 抑制剂。 |
| 生物活性 | Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor， with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ， respectively.[1-2] |
| In Vitro | Buparlisib (BKM120) exhibits 50-300 nM activity for class I PI3K’s， including the most common p110α mutants. Additionally， NVP-BKM120 exhibits 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[1]. Buparlisib (BKM120) induces multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. Buparlisib (BKM120) at concentrations ≥10 μM induces significant apoptosis in all tested MM cell lines at 24 h (P50 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 50 for U266 is between 10 and 100 μM. In summary， Buparlisib (BKM120) treatment results in MM cell growth inhibition and apoptosis in dose- and time-dependent manners[2]. |
| In Vivo | In A2780 xenograft tumors， oral dosing of Buparlisib (BKM120) at 3， 10， 30， 60， and 100 mg/kg results in a dose dependent modulation of pAKTSer473. 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]. Mice receiving Buparlisib (BKM120) (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice， which are measured as tumor volume (P[2]. |
| 细胞实验 | A2780 cells are cultured in DMEM supplemented with 10% FBS. L-glutamine， sodium pyruvate， and antibiotics. Cells are plated in the same medium at a density of 1000 cells per well， 100 uL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. Buparlisib (BKM120) supplied in DMSO (20 mM) are diluted further into DMSO (7.5 uL of 20 mM NVP-BKM120 in 22.5 uL DMSO. Mix well， transfer 10 uL to 20 uL DMSO， repeat until 9 concentrations have been made). The diluted Buparlisib (BKM120) solution (2 uL)， is then added to cell medium (500 uL) cell medium. Equal volumes of this solution (100 uL) are added to the cells in 96 well plates and incubated at 37oC for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux[1]. |
| 动物实验 | Mice[2]Six- to eight-week-old female severe combined immunodeficiency (SCID) mice are used. SCID mice are subcutaneously inoculated in the right flank with 1 million ARP-1 or MM.1S cells suspended in 50 μL phosphate-buffered saline (PBS). After palpable tumor developed (tumor diameter ≥5 mm)， mice are treated with intraperitoneal injection of DMSO/PBS or Buparlisib (BKM120) (5 μM per kg per day) for 15 days. Tumor sizes are measured every 5 days， and blood samples are collected at the same period. Tumor burdens are evaluated by measuring tumor size and detecting circulating human kappa chain or lambda chain. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
| 1mM-5mg | 11.1894mL |
| 1mM-1mg | 2.2379mL |
| 1mM-10mg | 22.3789mL |
| 5mM-1mg | 0.4476mL |
| 5mM-5mg | 2.2379mL |
| 5mM-10mg | 4.4758mL |
| 10mM-1mg | 0.2238mL |
| 10mM-5mg | 1.1189mL |
| 10mM-10mg | 2.2379mL |
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