Buparlisib (BKM120) | CAS:944396-07-0 | Manufacturer ChemFaces

Buparlisib (BKM120)

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Description:

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis.

Targets:

PI3K | VPS34 | mTOR | DNAPK

In vitro:

J Mol Med (Berl),2012 Jun;90(6):695-706.

Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone.[Pubmed: 22207485]

NVP-BKM120 is a novel phosphatidylinositol 3-kinase (PI3K) inhibitor and is currently being investigated in phase I clinical trials in solid tumors. This study aimed to evaluate the therapeutic efficacy of BKM120 in multiple myeloma (MM).
METHODS AND RESULTS:
BKM120 induces cell growth inhibition and apoptosis in both MM cell lines and freshly isolated primary MM cells. However, BKM120 only shows limited cytotoxicity toward normal lymphocytes. The presence of MM bone marrow stromal cells, insulin-like growth factor, or interleukin-6 does not affect BKM120-induced tumor cell apoptosis. More importantly, BKM120 treatment significantly inhibits tumor growth in vivo and prolongs the survival of myeloma-bearing mice. 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. Mechanistic study shows that 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 cytotoxic small isoform of Bim, BimS.
CONCLUSIONS:
In summary, our findings demonstrate the in vitro and in vivo anti-MM activity of BKM120 and suggest that BKM120 alone or together with other MM chemotherapeutics, particularly dexamethasone, may be a promising treatment for MM.

Buparlisib (BKM120) Description

Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Cell Research:

ACS Med. Chem. Lett.2011,2(10):774–779.

Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.[Reference: WebLink]

Cell lines:A2780 cells.
Concentrations: 0-6.6 μM
Incubation Time: 3 days
Method:
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 103 cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux.

Product Name	Buparlisib (BKM120)
Price:
CAS No.:	944396-07-0
Catalog No.:	CFN60065
Molecular Formula:	C₁₈H₂₁F₃N₆O₂
Molecular Weight:	410.39 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS
Similar structural:	Comparison
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library PI3K Inhibitor Library mTOR Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.4367 mL	12.1835 mL	24.3671 mL	48.7341 mL	60.9177 mL
5 mM	0.4873 mL	2.4367 mL	4.8734 mL	9.7468 mL	12.1835 mL
10 mM	0.2437 mL	1.2184 mL	2.4367 mL	4.8734 mL	6.0918 mL
50 mM	0.0487 mL	0.2437 mL	0.4873 mL	0.9747 mL	1.2184 mL
100 mM	0.0244 mL	0.1218 mL	0.2437 mL	0.4873 mL	0.6092 mL

CFN96612	trans-3'-O-Benzoyl-4'-O-methylkhellactone	23733-95-1	380.39	C₂₂H₂₀O₆
CFN60103	LGK-974 (WNT974)	1243244-14-5	396.44	C₂₃H₂₀N₆O
CFN93244	13-Oxyingenol dodecanoat	54706-70-6	546.74	C₃₂H₅₀O₇
CFN93217	alpha-Asarone	2883-98-9	208.25	C₁₂H₁₆O₃