NVP-BKM120 Hydrochloride

• CAT Number: I001197
• CAS Number: 1312445-63-8
• Molecular Formula: C18H22ClF3N6O2
• Molecular Weight: 446.85
• Purity: ≥95%
• Synonyms: 5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine hydrochloride
• Target: Apoptosis
• Solubility: DMSO ≥80mg/mL Water <1mg/mL Ethanol ≥20mg/mL
• Storage: Store at -20°C
• IC50: 52 nM/166 nM/116 nM/262 nM(p110α/β/δ/γ) [1]
• IUPAC Name: 5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine;hydrochloride
• InChI: InChI=1S/C18H21F3N6O2.ClH/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);1H
• InChIKey: DGPLYAXBXJXEID-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4.Cl

NVP-BKM120 Hydrochloride (Cat No.:I001197) is a selective inhibitor of class I phosphoinositide 3-kinase (PI3K), targeting all four isoforms (α, β, γ, δ) of the PI3K enzyme. By inhibiting PI3K, NVP-BKM120 blocks downstream signaling pathways involved in cell growth, survival, and metabolism, making it a promising candidate for cancer therapy, particularly in solid tumors and hematological malignancies. It has shown efficacy in preclinical studies for inhibiting tumor cell proliferation and inducing apoptosis. NVP-BKM120 is being investigated in clinical trials for its potential in treating various cancers, including breast and lung cancers.

Reference

[1]. Burger MT, et al. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett, 2011, 2 (10), 774–779.
[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), 2011 Dec 30.
[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.