PF-4989216
作者：齊岳
發(fā)布時間：2023-09-05
08:53:52
點擊數：
產品名稱：PF-4989216
產品描述：
| 產品描述 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. |
| 靶點活性 | Vps34:110 nM, p110β:142 nM, p110δ:1 nM, p110α:2 nM, p110γ:65 nM |
| 體外活性 | PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis. [1] |
| 體內活性 | In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity. [1] |
| 細胞實驗 | SCLC cells are cultured (5,000 cells/well) in a 96-well microtiter plate at 37°C in 5% CO2 in supplier-recommended growth media and compounds are added to each well starting at 10 μM with a 3-fold serial dilution. At 72 hours after compound addition, CellTiter-Glo (CTG) Solution is added per the manufacturer's instructions. Luminescence is read on an Envision plate reader. All experiments are run in duplicate and have been repeated at least three times.(Only for Reference) |
| 別名 | PF 4989216 |
| 分子量 | 380.4 |
| 分子式 | C18H13FN6OS |
| CAS No. | 1276553-09-3 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 7 mg/mL (18.4 mM),warmed
H2O: <1 mg/mL
DMSO: 71 mg/mL (186.6 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業(yè)務范圍包括化學試劑和產品的研發(fā)、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
