NVP-BKM120

NVP-BKM120

NVP-BKM120

Min.Order / FOB Price:Get Latest Price

100 Gram

FOB Price: USD 1.0000

  • Min.Order :100 Gram
  • Purity: 98%
  • Payment Terms : L/C

Keywords

NVP-BKM120 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine;NVP-BKM-120;5-(2,6-diMorpholinopyriMidin-4-yl)-4-(trifluoroMethyl)pyridin-2-aMine;BKM120 (NVP-BKM120);BKM120 (NVP-BKM120, Bup 944396-07-0

Quick Details

  • Appearance:off white powder
  • Application:CAS:944396-07-0; Small molecule inhibitors,
  • PackAge:100g,500g,1kg,25kg
  • ProductionCapacity:1000|Gram|Month
  • Storage:Dry seal
  • Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.
 
 
 

We are committed to provide excellence in researching, manufacturing and drug discovery process.
 
 
 

Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

 

Details:

NVP-BKM120(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) [1]
Target: 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 [1]. 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 [2]. 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 [3].
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 [1]. BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day1in ARP1 SCID mouse model, with prolonged survival [2].

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