BKM120 - CAS 944396-07-0
Catalog number: B0084-438224
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H21F3N6O2
Molecular Weight:
410.39
COA:
Inquire
Targets:
PI3K
Description:
BKM120, also called as buparlisib or NVP-BKM120, activity in a range of preclinical cancermodels, specifically inhbits class I PI3K isoforms, which blocks p110α (IC50 = 52 nM), p110β (IC50 = 166 nM), p110δ (IC50 = 116 nM) and p110γ (IC50 = 262 nM). And BKM120 displays little sensitive to Class III and Class IV PI3K's or PI4K.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-438224 200 mg $198 In stock
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Brife Description:
Specifically inhbits class I PI3K isoforms
Appearance:
White to off-white solid
Synonyms:
5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine; BKM120; buparlisib; NVP-BKM120; 944396-07-0; BKM 120; BKM-120; UNII-0ZM2Z182GD; 1202777-78-3; 944396-07-0; NVP-BKM120; Buparlisib; 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine; NVP-BKM-120; BKM120; BKM 120; BKM-120; UNII-0ZM2Z182GD; 1202777-78-3; CHEMBL2017974; CHEBI:71954; 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine; 5-[2,6-Di(Morpholin-4-Yl)pyrimidin-4-Yl]-4-(Trifluoromethyl)pyridin-2-Amine; C18H21F3N6O2; BKM120, BKM-120|; 2-Pyridinamine,5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-; 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-Pyridinamine
Solubility:
Soluble to ≥80mg/mL in DMSO, to <1.2mg/mL in Water, to ≥22mg/mL in Ethanol
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -42℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Boiling Point:
645.7±65.0 °C | Condition: Press: 760 Torr
Density:
1.382±0.06 g/cm3
InChIKey:
CWHUFRVAEUJCEF-UHFFFAOYSA-N
InChI:
1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23)
Canonical SMILES:
C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4
Current Developer:
Dana-Farber Cancer Institute; Emory University; Indiana University; Memorial Sloan-Kettering Cancer Center; National Cancer Institute (Canada); National Cancer Institute (USA); Novartis; Novartis Oncology; Ohio State University; Paoli-Calmettes-institute; Sarah Cannon Research Institute; Stanford University; University Hospital Tubingen; University of California at San Francisco
Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors
Jordi Rodon, Irene BrañaLillian L Siu, Maja J De Jonge, Natasha Homji, David Mills, Emmanuelle Di Tomaso, Celine Sarr, Lucia Trandafir, Cristian Massacesi, Ferry Eskens, Johanna C Bendell. Investigational New Drugs, August 2014, Vol. 32, Issue 4, pp. 670–681
Observations of hyperglycemia are indicative of PI3K pathway inhibition in patients treated with buparlisib, and demonstrate a potential role for metabolites such as Cpeptide as pharmacodynamic biomarkers. The analysis of glucose metabolism biomarkers presented here further supports the observation that buparlisib inhibits the PI3K pathway and perturbs glucose metabolism; however, due to the heterogeneous patient population and the limited numbers of patients treated at dose levels other than the MTD, a clear relationship between these biomarkers and the dose of buparlisib administered or the degree of pathway inhibition, was not established. Further work is ongoing to establish the utility of biomarkers such as C-peptide, as indicators of PI3K inhibitor activity.
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Chemical Structure

CAS 944396-07-0 BKM120

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