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| | Buparlisib Hydrochloride Basic information |
| Product Name: | Buparlisib Hydrochloride | | Synonyms: | NVP-BKM120 (Hydrochloride);BKM 120 hydrochloride;BKM120 hydrochloride;BKM-120 hydrochloride;5-(2,6-DiMorpholinopyriMidin-4-yl)-4-(trifluoroMethyl)pyridin-2-aMine hydrochloride;5-(2,6-Di-4-morpholinyl-4-pyrimidinyl)-4-(trifluoromethyl)-2-pyridinamine hydrochloride (1:1);BKM 120AAA;Buparlisib hydrochloride | | CAS: | 1312445-63-8 | | MF: | C18H22ClF3N6O2 | | MW: | 446.86 | | EINECS: | | | Product Categories: | API | | Mol File: | 1312445-63-8.mol |  |
| | Buparlisib Hydrochloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | ≥44.7 mg/mL in DMSO; ≥52.8 mg/mL in H2O with gentle warming; ≥96 mg/mL in EtOH with gentle warming | | form | solid | | color | White to yellow | | 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 | C(C1=CC(N)=NC=C1C1=NC(N2CCOCC2)=NC(N2CCOCC2)=C1)(F)(F)F.Cl |
| | Buparlisib Hydrochloride Usage And Synthesis |
| Uses | NVP-BKM 120-d16 Hydrochloride is the salt, labeled analogue of NVP-BKM 120 (N925760), 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 |
Buparlisib hydrochloride (BKM120 Hydrochloride) is an investigational small molecule orally available pan-class I phosphoinositide 3-kinase inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
| | Mode of action |
Buparlisib specifically inhibits class I PIK3 in the PI3K/AKT kinase signaling pathway in an ATP-competitive manner, thus inhibiting the production of the secondary messenger phosphatidylinositol (3,4,5)-trisphosphate and activation of the PI3K signaling pathway. This may induce inhibition of tumour cell growth and survival in susceptible tumour cell populations. Buparlisib is currently under investigation in patients with a variety of solid tumours, including breast cancer[1].
| | References |
[1] Carmen Criscitiello. “Profile of buparlisib and its potential in the treatment of breast cancer: evidence to date.” Breast Cancer?: Targets and Therapy 10 (2018): 23–29.
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| | Buparlisib Hydrochloride Preparation Products And Raw materials |
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