Network Version
Acalisib Data Sheet
| Product Name: | Acalisib |
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|---|---|---|
| CAS No.: | 870281-34-8 | |
| Cat. No.: | HY-12644 | |
| MWt: | 401.4 | |
| Formula: | C21H16FN7O | |
| Purity : | >98% | |
| Solubility: | DMSO : 125 mg/mL (311.41 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM. IC50 & Target: IC50: 12.7 nM (PI3Kδ), 1389 nM (PI3Kγ), 3377 nM (PI3Kβ), 5441 nM (PI3Kα)[1] In Vitro: Acalisib (GS-9820) is more selective for PI3Kδ (IC50=12.7 nM) relative to other PI3K class I enzymes (IC50: PI3Kα, 5,441 nM; PI3Kβ, 3,377 nM; PI3Kγ, 1,389 nM). Acalisib is also 103-fold more selective against PI3Kδ than against related kinases, such as PI3KCIIβ (IC50>10 nM), hVPS34 (IC50=12.7 μM), DNA-PK (IC50=18.7 μM), and mTOR (IC50>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: 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[2]. | ||
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