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NVP-BKM120 Hydrochloride

HY-15180

(BKM-120 hydrochloride; BKM120 hydrochloride; BKM 120 hydrochloride)

NVP-BKM120 Hydrochloride

NVP-BKM120 Hydrochloride Chemical Structure

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.

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10 mM * 1 mL in DMSO $77 In-stock
5 mg $70 In-stock
10 mg $99 In-stock
50 mg $170 In-stock
100 mg $300 In-stock
200 mg Get quote
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Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €75 In-stock
5 mg €69 In-stock
10 mg €97 In-stock
50 mg €167 In-stock
100 mg €294 In-stock
200 mg Get quote
500 mg Get quote

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

NVP-BKM120 Hydrochloride Data Sheet

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    Purity: 98.60%

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Biological Activity of NVP-BKM120 Hydrochloride

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].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 446.85 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C18H22ClF3N6O2
CAS No 1312445-63-8
Solvent & Solubility

DMSO ≥80mg/mL Water <1mg/mL Ethanol ≥20mg/mL

Preparing Stock Solutions

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

Clinical Information of NVP-BKM120 Hydrochloride

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

References on NVP-BKM120 Hydrochloride

Other Forms

Inhibitor Kit

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