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Products are for research use only. Not for human use. We do not sell to patients.
(BKM-120 hydrochloride; BKM120 hydrochloride; BKM 120 hydrochloride)
NVP-BKM120 Hydrochloride Chemical Structure
|Product name: NVP-BKM120 Hydrochloride|
|Cat. No.: HY-15180|
NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.
IC50 value: 52 nM/166 nM/116 nM/262 nM(p110α/β/δ/γ) 
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 .
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 .
|M.Wt||446.85||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥80mg/mL Water <1mg/mL Ethanol ≥20mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.2379 mL||11.1894 mL||22.3789 mL|
|5 mM||0.4476 mL||2.2379 mL||4.4758 mL|
|10 mM||0.2238 mL||1.1189 mL||2.2379 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|NVP-BKM120 Hydrochloride||Novartis AG||Metastatic breast cancer||31-AUG-12||31-MAR-17||Phase 3||21-NOV-13|
|Novartis AG||Uterine cervix tumor||31-JAN-14||30-JUN-15||Phase 4||25-NOV-13|
|Novartis AG||Metastatic breast cancer||31-OCT-12||31-OCT-16||Phase 3||08-AUG-13|
|Washington University in St Louis||Breast tumor||31-JAN-14||31-JUL-15||Phase 2||17-OCT-13|
|Novartis AG||Breast tumor||30-NOV-13||31-MAY-16||Phase 2||12-SEP-13|
. 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), 2011 Dec 30.
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