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Buparlisib (BKM120) - 10mM in DMSO, high purity , CAS No.944396-07-0(DMSO), PI3-kinase class I inhibitor

COA

Grade & Purity:

Moligand™

10mM in DMSO

Cas Number: 944396-07-0(DMSO)
Molecular Weight: 410.39

In stock

Item Number

B408526

Grouped product items
SKU	Size	Availability	Price	Qty
B408526-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$277.90

p110β Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	NVP-BKM120 \| 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
Specifications & Purity	Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms	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
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	PI3-kinase class I inhibitor
Product Description	Information Buparlisib (BKM120, NVP-BKM120) is a selectivePI3Kinhibitor ofp110α/β/δ/γwithIC50of 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 inducesapoptosis. Phase In vitro BKM120 is not sensitive to Class III and Class IV PI3K\'s or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM. BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138− stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP. BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells. A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. In vivo BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg. BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day−1in ARP1 SCID mouse model, with prolonged survival. Cell Data cell lines：A number of tumor cell lines, including BT20, MCF-7, DU145, PC3, U87, A549, H187, RF1, HCT15, HeLa, and Raji cells Concentrations：0-6.6 μM Incubation Time：3 days. Powder Purity:≥99%

Product Properties

ALogP	2.342
hba_count	5
HBD Count	1
Rotatable Bond	4

Associated Targets(Human)

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (5 Activities)

Discover Target: PIK3CA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR (1 Activities)

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	NC1=CC(=C(C=N1)C2=NC(=NC(=C2)N3CCOCC3)N4CCOCC4)C(F)(F)F
Molecular Weight	410.39
Reaxy-Rn	12938097
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12938097&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 92 mg/mL (199.57 mM); Ethanol: 92 mg/mL (199.57 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	82
DMSO(mM) Max Solubility	199.81
Water(mg / mL) Max Solubility	<1

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