成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

返回ChemicalBook首頁>CAS數(shù)據(jù)庫列表>870281-34-8

870281-34-8

中文名稱 GS-9820
英文名稱 GS-9820
CAS 870281-34-8
分子式 C21H16FN7O
分子量 401.4
MOL 文件 870281-34-8.mol
更新日期 2024/11/13 09:55:59
870281-34-8 結(jié)構(gòu)式 870281-34-8 結(jié)構(gòu)式

基本信息

中文別名
PI3KΔ抑制劑(ACALISIB)
英文別名
GS-9820
CS-1758
Acalisib
UNII-OVW60IDW1D
Acalisib (GS-9820)
Acalisib(GS9820,CAL-120)
UNII-OVW60IDW1D
ACALISIB (GS-9820)

6-Fluoro-3-phenyl-2-[1-(7H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone
6-Fluoro-3-phenyl-2-[(1S)-1-(1H-purin-6-ylamino)ethyl]-4(3H)-quinazolinone
4(3H)-Quinazolinone, 6-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)ethyl]-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點733.7±70.0 °C(Predicted)
密度1.50±0.1 g/cm3(Predicted)
儲存條件4°C, protect from light
溶解度insoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL in DMSO
酸度系數(shù)(pKa)10.01±0.10(Predicted)
形態(tài)固體
顏色White to off-white

圖譜信息

常見問題列表

生物活性
Acalisib (GS-9820, CAL-120)是一種具有高度選擇性的、有效的p110δ抑制劑,IC50為14 nM。它對p110δ的選擇性是對其他I類PI3K酶的選擇性的114-400倍,對II類和III類PI3K酶和其他PI3K相關(guān)蛋白(包括mTOR和DNA-PK)沒有活性。
靶點
TargetValue
p110δ
()
14 nM
體外研究

Acalisib (GS-9820) is more selective for PI3Kδ (IC 50 =12.7 nM) relative to other PI3K class I enzymes (IC 50 : PI3Kα, 5,441 nM; PI3Kβ, 3,377 nM; PI3Kγ, 1,389 nM). Acalisib is also 10 3 -fold more selective against PI3Kδ than against related kinases, such as PI3KCIIβ (IC 50 >10 nM), hVPS34 (IC 50 =12.7 μM), DNA-PK (IC 50 =18.7 μM), and mTOR (IC 50 >10 nM). In fibroblasts, the PDGF receptor signals through PI3Kα and the GPCR for lysophosphatidic acid (LPA) signals through PI3Kβ. Acalisib reduces PDGF-induced pAkt by only 50% at 11,585 nM, and LPA-induced pAkt by 50% at 2,069 nM.

體內(nèi)研究

To dissect the relative contribution of PI3Kα and PI3Kδ inhibition in the reduction of obesity, obese hyperphagic ob/ob mice are treated with a selective PI3Kα inhibitor, BYL-719, or with a selective PI3Kδ inhibitor, Acalisib (GS-9820). Remarkably, BYL-719 reduces body weight after 15 days of treatment to a similar extent as CNIO-PI3Ki, whereas Acalisib has no significant effect at the same doses as BYL-719. It should be noted that 10 mg/kg of Acalisib is sufficient to reduce the growth of multiple myeloma xenografts in mice.

"870281-34-8" 相關(guān)產(chǎn)品信息
90028-66-3