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Cat. No. Name Size Price Add Cart
KI1319BKM1205 mg$272
BKM12010 mg$300
BKM12050 mg$988

Chemical Characteristic

Product NameBKM120
SynonymsNVP-BKM120
CAS No.944396-07-0
Molecular Weight 410.39
FormulaC18H21F3N6O2
Chemical Name5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
Smilesc1(cc(c(cn1)c1nc(nc(c1)N1CCOCC1)N1CCOCC1)C(F)(F)F)N
Chemical Structure

Biological activities

BKM120 is an available pan-Class I PI3-kinase inhibitor. The IC50 of BKM120 is 52, 58 and 99 nM against p110α, p110α-H1047R and p110α-E545K, respectively. In contrast, BKM120 inhibits p110β, p110δ and p110γ with IC50 of 166,116 and 262 nM, respectively. BKM120 prevents the activities of PI3Kα via a mixed-type mode, affecting both the Vmax and the Km for ATP. BKM120 is significantly less potent in biochemical assays against the PI3K class III family member Vps34, the related class IV PIKK protein kinases mTOR, ATR, and DNA-PK, and the distinct lipid kinase PI4Kβ. BKM120 inhibits S473P-Akt in a concentration-dependent manner with IC50 values (RPPA determination) of 104, 234, and 463 nM in cell lines that express myr-p110α, p110β, and p110δ, respectively. BKM120 decreases not only S473P-Akt but also T308P-Akt levels, with IC50 of 130 and 229 nM, respectively, in PTEN-null U87MG cells.[1] BKM120 induces cell growth inhibition and apoptosis in both multiple myeloma (MM) cell lines and freshly isolated primary MM cells.[2] In KRAS mutant gastric cancer cells, either p-ERK or p-STAT3 is increased upon treatment of BKM120.[3] BKM120 preferentially inhibits tumor cells bearing oncogenic mutations in the PIK3CA gene. BKM120 efficiently inhibits the PI3K pathway in tumor-bearing animals and displays strong antitumor activity in vivo.[1] In another study, BKM120 significantly inhibits tumor growth in vivo and prolongs the survival of myeloma-bearing mice.[2]

Protocols

In vitro: BKM120 is prepared as 10 mM stock solutions in 100% dimethyl sulfoxide (DMSO).[1]

References

[1] Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther. 2012, 11(2): 317-328.
[2] Zheng Y, et al. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone. J Mol Med (Berl). 2012, 90(6): 695-706.
[3] Park E, et al. NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations.Int J Oncol. 2012, 40(4): 1259-1266.

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