1. PI3K/Akt/mTOR
  2. PI3K

NVP-BKM120 Hydrochloride (Synonyms: BKM-120 hydrochloride; BKM120 hydrochloride; BKM 120 hydrochloride)

Cat. No.: HY-15180 Purity: 98.60%
Handling Instructions

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.

For research use only. We do not sell to patients.
NVP-BKM120 Hydrochloride Chemical Structure

NVP-BKM120 Hydrochloride Chemical Structure

CAS No. : 1312445-63-8

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
5 mg $60 In-stock
10 mg $90 In-stock
50 mg $150 In-stock
100 mg $250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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) [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/day?1in ARP1 SCID mouse model, with prolonged survival [2].

Clinical Trial
Sponsor Condition Start Date Phase
Novartis AG Uterine cervix tumor 2014-01-31 Phase 4
Novartis AG Metastatic breast cancer 2012-10-31 Phase 3
Novartis AG Metastatic breast cancer 2012-08-31 Phase 3
Washington University in St Louis Breast tumor 2014-01-31 Phase 2
Novartis AG Breast tumor 2013-11-30 Phase 2
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 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
M.Wt

446.85

Formula

C₁₈H₂₂ClF₃N₆O₂

CAS No.

1312445-63-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 98.60%

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Product Name:
NVP-BKM120 Hydrochloride
Cat. No.:
HY-15180
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