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Idelalisib

Chemical Structure : Idelalisib

CAS No.: 870281-82-6

Idelalisib (CAL-101;GS-1101;GS1101;GS1101)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 415.423
Formula C22H18FN7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 59.7 mg/mL

Chemical Name/SMILES

4(3H)-Quinazolinone, 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-

References

1. Hoellenriegel J, et al. Blood. 2011 Sep 29;118(13):3603-12.

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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