Chemical Structure : Idelalisib
CAS No.: 870281-82-6
货号: PC-43336Not For Human Use, Lab Use Only.
Idelalisib (CAL-101, GS-1101) is a potent, selective inhibitor of PI3K p110δ with IC50 of 2.5 nM, 40- to 300-fold selectivity over other class I PI3Ks (p110α/βγ, IC50=820/565/89nM), and 400- to 4000-fold over C2β, hVPS34, DNA-PK, and mTOR.
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Idelalisib (CAL-101, GS-1101) is a potent, selective inhibitor of PI3K p110δ with IC50 of 2.5 nM, 40- to 300-fold selectivity over other class I PI3Ks (p110α/βγ, IC50=820/565/89nM), and 400- to 4000-fold over C2β, hVPS34, DNA-PK, and mTOR.
Idelalisib (CAL-101, GS-1101) blocks FcϵRI p110δ-mediated CD63 expression in basophils with an EC50 of 8 nM.
Idelalisib (CAL-101, GS-1101) blocks constitutive PI3K signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in PARP and caspase cleavage and an induction of apoptosis in multiple B-cell malignancies.
分子量 | 415.423 | |
分子式 | C22H18FN7O | |
外观性状 | Solid | |
储存条件 |
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Solubility |
DMSO: ≥ 59.7 mg/mL |
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Chemical Name/SMILES |
4(3H)-Quinazolinone, 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]- |
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2. Herman SE, et al. Blood. 2010 Sep 23;116(12):2078-88.
3. Lannutti BJ, et al. Blood. 2011 Jan 13;117(2):591-4.
4. Bodo J, et al. Br J Haematol. 2013 Oct;163(1):72-80.
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