BEZ235 , ≥99% , 915019-65-7

CAS NO.：915019-65-7

Empirical Formula: C30H23N5O

Molecular Weight: 469.55

MDL number: MFCD10565944

EINECS: 1312995-182-4

PRODUCT Properties

• Melting point: 288-289°C
• Boiling point: 701.0±70.0 °C(Predicted)
• Density: 1.299
• storage temp.: Refrigerator
• solubility: Soluble in DMSO (up to 1 mg/ml with warming) or in DMF (up to 10 mg/ml, dissolves slowly, requires heating to 75C).
• form: White powder.
• pka: 6.41±0.20(Predicted)
• color: White or off-white
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 1 month.
• InChI: InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3
• InChIKey: JOGKUKXHTYWRGZ-UHFFFAOYSA-N
• SMILES: O=C1N(C2C=NC3=CC=C(C4C=NC5C=CC=CC=5C=4)C=C3C=2N1C1C=CC(C(C)(C)C#N)=CC=1)C
• CAS DataBase Reference: 915019-65-7

Description and Uses

NVP-BEZ235 (915019-65-7) is a dual PI3K and mTOR kinase inhibitor.1It inhibits VEGF-induced proliferation and angiogenesis.2Reverses lapatinib resistance.3It induces G1 arrest and reduces cyclin D1 expression in melanoma cells with negligible apoptosis.4NVP-BEZ235 inhibits the growth of cancer cells with activating PI3K mutations.5The ability of NVP-BEZ235 to inhibit PI3K has come into question. This study also shows it to be a potent inhibitor of PRKDC (IC50 = 29 nM), ATM (IC50 = 13 nM), and ATR (IC50 = 8 nM).6Active in vivo.

Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. NVP-BEZ235 is a potent dual inhibitor of PI3K and mTOR that is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents when used in in vivo combination studies. It inhibits PI3K isoforms and mutants with low nanomolar IC50 values, leading to growth arrest in the G1 phase. Through its effects on PI3K, NVP-BEZ235 inhibits VEGF-induced angiogenesis. By directly blocking cell growth and indirectly inhibiting angiogenesis, it has potential in both solid tumors and in metastatic melanoma therapy.[Cayman Chemical]

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338