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Buparlisib

Catalog No. T1827 CAS 944396-07-0

Synonyms: BKM120, NVP-BKM120

Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).

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Buparlisib, CAS 944396-07-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 57.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 95.00
50 mg	In stock	$ 117.00
100 mg	In stock	$ 147.00
200 mg	In stock	$ 247.00
500 mg	In stock	$ 447.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 98.4%

Purity: 98%

Purity: 96.22%

Purity: 95.32%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).
Targets&IC50	p110α:52 nM (cell free), p110γ:262 nM (cell free), p110δ:116 nM (cell free), p110β:166 nM (cell free), VPS34:2.4 μM (cell free)
In vitro	Buparlisib exhibited 50-300 nM activity for class I PI3K's, including the most common p110R mutants. Additionally, 15 exhibited lower potency against class III and class IV PI3K's, where 2, 5, >5, and >25 μM biochemical activity was observed for inhibition of VPS34, mTOR, DNAPK, and PI4K, respectively. Across all cell lines, pathway modulation and antiproliferative activity was consistent with cellular PI3K inhibition [1]. Buparlisib demonstrated anti-proliferative activity in 11 human gastric cancer cell lines by decreasing mTOR downstream signaling. But Buparlisib treatment increased p-AKT by subsequent abrogation of feedback inhibition by stabilizing insulin receptor substrate-1. In KRAS mutant gastric cancer cells, either p-ERK or p-STAT3 was also increased upon treatment of Buparlisib [2]. BKM120 induces cell growth inhibition and apoptosis in both multiple myeloma (MM) cell lines and freshly isolated primary MM cells. In addition, BKM120 shows synergistic cytotoxicity with dexamethasone in dexamethasone-sensitive MM cells. Low doses of BKM120 and dexamethasone, each of which alone has limited cytotoxicity, induce significant cell apoptosis in MM.1S and ARP-1. BKM120 exposure causes cell cycle arrest by upregulating p27 (Kip1) and downregulating cyclin D1 and induces caspase-dependent apoptosis by downregulating antiapoptotic XIAP and upregulating expression of a cytotoxic small isoform of Bim, BimS [3].
In vivo	In A2780 xenograft tumors, oral dosing of Buparlisib at 3, 10, 30, 60, and 100 mg/kg resulted in a dose-dependent modulation of pAKTSer473. Partial inhibition of pAKTser473 was observed at 3 and 10 mg/kg, and near complete inhibition was observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAkt tracked well with both plasma and tumor drug exposure. pAKT modulation was also time-dependent, with >90% target modulation achieved with the 60 and 100 mg/kg dose at the 10 h time point when the plasma and tumor exposure was ca. 2 μM [1]. The treatment by Buparlisib (5 μM/kg/day) had significantly smaller tumor burdens as compared with control mice, which were measured as tumor volume and level of circulating human kappa chain. In addition, Buparlisib treatment significantly prolonged the survival of tumor-bearing mice [3].
Kinase Assay	Compounds to be tested were dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 μL per well. To start the reaction, 25 μL of 10 nM PI3 kinase and 5 μg/mL 1-alpha-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) were added into each well followed by 25 μL of 2 μM ATP in assay buffer. The reaction was performed until approx 50% of the ATP was depleted, and then stopped by the addition of 25 μL of KinaseGlo solution. The stopped reaction was incubated for 5 minutes and the remaining ATP was then detected via luminescence [1].
Cell Research	A2780 cells were cultured in DMEM supplemented with 10% FBS. L-glutamine, sodium pyruvate, and antibiotics. Cells were 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. Test compounds supplied in DMSO (20 mM) were diluted further into DMSO (7.5 ul of 20 mM test compound in 22.5 ul DMSO. Mix well, transfer 10 ul to 20 ul DMSO, repeat until 9 concentrations have been made). The diluted test compound solution (2uL), was then added to the cell medium (500 ul) cell medium. Equal volumes of this solution (100 uL) were added to the cells in 96 well plates and incubated at 37 oC for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation was determined by luminescence read using Trilux [1].
Animal Research	Six- to eight-week-old female severe combined immunodeficiency (SCID) mice were housed and monitored in the MD Anderson Cancer Center animal research facility. SCID mice were 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 were treated with intraperitoneal injection of DMSO/PBS or BKM120 (5 μM per kg per day) for 15 days. Tumor sizes were measured every 5 days, and blood samples were collected at the same period. Tumor burdens were evaluated by measuring tumor size and detecting the circulating human kappa chain or lambda chain [3].

Synonyms	BKM120, NVP-BKM120
Molecular Weight	410.39
Formula	C18H21F3N6O2
CAS No.	944396-07-0

Storage

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

Solubility Information

DMSO: 76 mg/mL (185.2 mM)

H2O: Insoluble

Ethanol: 2 mg/mL

References and Literature

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. Park E, et al. NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations. Int J Oncol. 2012 Apr;40(4):1259-66. 3. 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. 4. Hu P, Li H, Yu X, et al. GL-V9 exerts anti-T cell malignancies effects via promoting lysosome-dependent AKT1 degradation and activating AKT1/FOXO3A/BIM axis[J]. Free Radical Biology and Medicine. 2019. 5. Wencao Zhao, Le Cao, Hanru Ying, Wenjuan Zhang, Dantong Li, Xiaolong Zhu, Wenzhi Xue, Shuang Wu, Mengye Cao, Cong Fu, Haonan Qi, Yimei Hao, Yun-Chi Tang, Jun Qin, Tao P. Zhong, Xiaoxi Lin, Luyang Yu, Xuri Li, Lin Li, Dianqing Wu & Weijun Pan . Endothelial CDS2 deficiency causes VEGFA-mediated vascular regression and tumor inhibition. Cell Research. 2019

Citations

1. Wencao Zhao, Le Cao, Hanru Ying, Wenjuan Zhang, Dantong Li, Xiaolong Zhu, Wenzhi Xue, Shuang Wu, Mengye Cao, Cong Fu, Haonan Qi, Yimei Hao, Yun-Chi Tang, Jun Qin, Tao P. Zhong, Xiaoxi Lin, Luyang Yu, Xuri Li, Lin Li, Dianqing Wu & Weijun Pan Endothelial CDS2 deficiency causes VEGFA-mediated vascular regression and tumor inhibition. Cell Research. 2019 2. Hu P, Li H, Yu X, et al. GL-V9 exerts anti-T cell malignancies effects via promoting lysosome-dependent AKT1 degradation and activating AKT1/FOXO3A/BIM axis. Free Radical Biology and Medicine. 2019

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Antidepressant Compound Library Orally Active Compound Library Anti-Metabolism Disease Compound Library Metabolism Compound Library

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Keywords

Buparlisib 944396-07-0 Apoptosis PI3K/Akt/mTOR signaling PI3K BKM120 Phosphoinositide 3-kinase inhibit BKM 120 Inhibitor NVP-BKM-120 BKM-120 NVP-BKM120 NVP-BKM 120 inhibitor

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