DC Chemicals Limited
China
Product Name: BGT-226
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

915020-55-2

915020-55-2 structure

Name: BGT226 free base
Chemical Name: 8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one
CAS Number: 915020-55-2
Molecular Formula: C₂₈H₂₅F₃N₆O₂
Molecular Weight: 534.53
Catalog: Signaling Pathways Autophagy Autophagy
Create Date: 2018-12-24 21:16:58
Modify Date: 2024-01-05 09:11:49
BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells[1][2].

Name	8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one
Synonyms	8-(6-Methoxy-3-pyridinyl)-3-methyl-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one 2H-Imidazo[4,5-c]quinolin-2-one, 1,3-dihydro-8-(6-methoxy-3-pyridinyl)-3-methyl-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]- BGT226 free base BGT-226 free base 8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one 8-(6-Methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one UNII-ZXE7F2GMJJ

Description	BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells[1][2].
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> mTOR Research Areas >> Cancer Signaling Pathways >> PI3K/Akt/mTOR >> PI3K Signaling Pathways >> Autophagy >> Autophagy
Target	PI3Kα:4 nM (IC50) PI3Kβ:63 nM (IC50) PI3Kγ:38 nM (IC50) mTOR Autophagy
In Vitro	BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively[2]. The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines[2]. Cell Viability Assay[2] Cell Line: FaDu cells; OECM1 cells Concentration: 10, 100, 1000, 10000 nM Incubation Time: Result: Inhibited FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively. Western Blot Analysis[2] Cell Line: FaDu cells; OECM1 cells Concentration: 200 nM Incubation Time: 24 hours Result: p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased.
In Vivo	BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control[2]. Animal Model: Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model[2] Dosage: 2.5 and 5 mg/kg Administration: Oral administration; 21 days Result: Caused 34.7% and 76.1% reduction of the tumor growth.
References	[1]. Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408. [2]. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26.

Density	1.4±0.1 g/cm3
Boiling Point	713.3±70.0 °C at 760 mmHg
Molecular Formula	C₂₈H₂₅F₃N₆O₂
Molecular Weight	534.53
Flash Point	385.2±35.7 °C
Exact Mass	534.199097
PSA	77.21000
LogP	3.41
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.628

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