Acalisib(GS9820,CAL-120)

Name	Acalisib
Synonyms	GS-9820 Acalisib Acalisib (GS-9820) Acalisib(GS9820,CAL-120) 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 6-fluoro-3-phenyl-2-[(1S)-1-[(9H-purin-6-yl)amino]ethyl]-3,4-dihydroquinazolin-4-one (S)-2-(1-((7H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one Acalisib (GS-9820)
CAS	870281-34-8
EINECS	604-604-1

Molecular Formula	C21H16FN7O
Molar Mass	401.4
Density	1.50±0.1 g/cm3(Predicted)
Boling Point	733.7±70.0 °C(Predicted)
Solubility	DMSO: ≥ 29 mg/mL
pKa	10.01±0.10(Predicted)
Storage Condition	-20℃
In vitro study	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.
In vivo study	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.

Last Update：2024-01-02 23:10:35

Product Name: Acalisib Visit Supplier Webpage Request for quotation
CAS: 870281-34-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

Product Name: Acalisib Visit Supplier Webpage Request for quotation
CAS: 870281-34-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

View History

Acalisib(GS9820,CAL-120)

Acalisib(GS9820,CAL-120) Request for Quotation