ChemicalBook > CAS DataBase List > BKM120 (NVP-BKM120, Buparlisib)

BKM120 (NVP-BKM120, Buparlisib)

Product Name
BKM120 (NVP-BKM120, Buparlisib)
CAS No.
944396-07-0
Chemical Name
BKM120 (NVP-BKM120, Buparlisib)
Synonyms
isib;100821;CS-227;BuparL;AN-2025;Buparlisib;BKM120BASE;NVP-BKM-120;BKM120, >=98%;NVP-BKM120, BKM120
CBNumber
CB82509983
Molecular Formula
C18H21F3N6O2
Formula Weight
410.39
MOL File
944396-07-0.mol
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BKM120 (NVP-BKM120, Buparlisib) Property

Melting point:
143-147°C
Boiling point:
645.7±65.0 °C(Predicted)
Density 
1.382
storage temp. 
-20°C
solubility 
Soluble in DMSO (15 mg/ml)
form 
White powder.
pka
5.94±0.50(Predicted)
color 
White
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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Safety

HS Code 
29349990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H341Suspected of causing genetic defects

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P281Use personal protective equipment as required.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
11587
Product name
NVP-BKM120
Purity
≥95%
Packaging
5mg
Price
$26
Updated
2024/03/01
Cayman Chemical
Product number
11587
Product name
NVP-BKM120
Purity
≥95%
Packaging
50mg
Price
$141
Updated
2024/03/01
Cayman Chemical
Product number
11587
Product name
NVP-BKM120
Purity
≥95%
Packaging
1mg
Price
$31
Updated
2023/06/20
Cayman Chemical
Product number
11587
Product name
NVP-BKM120
Purity
≥95%
Packaging
10mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
11587
Product name
NVP-BKM120
Purity
≥95%
Packaging
25mg
Price
$102
Updated
2024/03/01
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BKM120 (NVP-BKM120, Buparlisib) Chemical Properties,Usage,Production

Description

Buparlisib (944396-07-0) is potent pan-Class I PI3-kinase inhibitor (IC50’s: p110α = 52 nM, p110? = 166 nM, p110δ = 116 nM. P110g = 262 nM).1,2 It inhibited microtubule dynamics at in vitro concentrations >1μM and doses above 50mg/kg in mice.3 Buparlisib lead to a precipitous drop in DNA synthesis in a mouse model of BRCA1-linked triple-negative breast cancer with less affect in normal tissue.4

Uses

A selective Class I PI3K inhibitor of p110α, p110β, p110δ and p110γ with IC50s of 50-300 nM.

Uses

NVP-BKM 120 is a novel anti-tumor active compound that is selective in that it inhibits specifically PI3 kinase activating cell death in glioma cells. Glioma cells being those that proliferate from tumors in the brain or the spine.

Definition

ChEBI: BKM120 is an aminopyridine that is 4-(trifluoromethyl)pyridin-2-amine substituted at position 5 by a 2,6-di(morpholin-4-yl)pyrimidin-4-y group. A selective PI3K inhibitor with anti-tumour properties. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an antineoplastic agent. It is a member of morpholines, an aminopyrimidine, an aminopyridine and an organofluorine compound.

in vivo

In A2780 xenograft tumors, oral dosing of Buparlisib (NVP-BKM120) at 3, 10, 30, 60, and 100 mg/kg results in a dose dependent modulation of pAKTSer473. Partial inhibition of pAKTSer473 is observed at 3 and 10 mg/kg, and near complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma and tumor drug exposure[1]. Mice receiving Buparlisib (NVP-BKM120) (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice, which are measured as tumor volume (P<0.05) and level of circulating human kappa chain (P<0.05). In addition, NVP-BKM120 treatment significantly prolongs the survival of tumor-bearing mice (P<0.05)[2].

target

p110α

IC 50

p110α: 52 nM (IC50); p110α-H1047R: 58 nM (IC50); p110α-E545K: 99 nM (IC50); p110δ: 116 nM (IC50); p110β: 166 nM (IC50); p110γ: 262 nM (IC50); Vps34: 2.4 μM (IC50); mTOR: 4.6 μM (IC50)

References

[1] MATTHEW T. BURGER*. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer[J]. ACS Medicinal Chemistry Letters, 2011, 2 10: 774-779. DOI:10.1021/ml200156t
[2] SAUVEUR-MICHEL MAIRA. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.[J]. Molecular Cancer Therapeutics, 2012, 11 2: 317-328. DOI:10.1158/1535-7163.mct-11-0474
[3] SASKIA M BRACHMANN. Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations.[J]. Molecular Cancer Therapeutics, 2012, 11 8: 1747-1757. DOI:10.1158/1535-7163.mct-11-1021
[4] ASHISH JUVEKAR. Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2016, 113 30: E4338-47. DOI:10.1073/pnas.1522223113

BKM120 (NVP-BKM120, Buparlisib) Preparation Products And Raw materials

Raw materials

Preparation Products

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BKM120 (NVP-BKM120, Buparlisib) Suppliers

Canada 1 China 204 India 2 United Kingdom 2 United States 24 Global 233
Shanghai Boyle Chemical Co., Ltd.
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J & K SCIENTIFIC LTD.
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Chembest Research Laboratories Limited
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+86-21-20908456
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021-58180499
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Jia Xing Isenchem Co.,Ltd
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0573-85285100 18627885956
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Nanjing Chemlin Chemical Co., Ltd
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025-83697070
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+86-25-83453306
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China DongFan Chemical Co.,LTD
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Jinan Trio PharmaTech Co., Ltd.
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Nanjing Vital Chemical Co., Ltd.
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chemweiao@163.com
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
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Shanghai Hope Chem Co., Ltd.，
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View Lastest Price from BKM120 (NVP-BKM120, Buparlisib) manufacturers

Zhejiang J&C Biological Technology Co.,Limited
Product
NVP-BKM-120 944396-07-0
Price
US $0.00/gram
Min. Order
1gram
Purity
99%
Supply Ability
10kg
Release date
2022-02-17
Career Henan Chemical Co
Product
BKM120 (NVP-BKM120, Buparlisib) 944396-07-0
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

944396-07-0, BKM120 (NVP-BKM120, Buparlisib)Related Search:

Epacadostat (INCB024360) Nintedanib Ethanesulfonate Salt AnaMorelin hydrochloride Niraparib tosylate MK-4827 (tosylate) Everolimus MK-2206 2HCl Alpelisib (BYL719) Pictilisib CAL-101 BEZ235 (NVP-BEZ235, Dactolisib) Ruxolitinib phosphate R428 Nutlin 3a 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline 6-Amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide BMS-794833 EGF816 (mesylate)

  • 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine
  • 5-(2,6-diMorpholinopyriMidin-4-yl)-4-(trifluoroMethyl)pyridin-2-aMine
  • BKM120 (NVP-BKM120)
  • NVP-BKM-120
  • BKM120 (NVP-BKM120, Buparlisib)
  • NVP-BKM120, Buparlisib
  • BKM120BASE
  • Buparlisib
  • BKM-120 4-(2,6-diMorpholinopyriMidin-4-yl)-3-(trifluoroMethyl)aniline
  • 5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
  • AN-2025
  • 100821
  • CS-227
  • NVP-BKM120,Buparlisib,BKM120, >98%
  • NVP-BKM-120; BKM-120; BUPARLISIB
  • 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine BKM120 (NVP-BKM120, Buparlisib)
  • NVP-BKM-120 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine
  • NVP-BKM120, BKM120
  • BKM120, >=98%
  • BKM120 (Buparlisib)
  • 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine BKM120
  • 2-Pyridinamine, 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-
  • Buparlisib, 98%, a selective PI3K inhibitor
  • Buparlisib (BKM120, NVP-BKM120)
  • NVP-BKM-120; BKM-120;BUPARLISIB;BKM120;BKM 120
  • BuparL
  • isib
  • BKM120 (NVP-BKM120, Buparlisib) USP/EP/BP
  • NVP-BKM120，Buparlisib，BKM120
  • Buparlisib, 10 mM in DMSO
  • 944396-07-0
  • C18H21O2N6F3
  • C18H21F3N6O2
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
  • Inhibitor
  • API