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Idelalisib (CAL-101,GS-1101)

  Cat. No.:  DC5068   Featured
Chemical Structure
870281-82-6
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Field of application
CAL-101 is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 870281-82-6
Chemical Name: (S)-2-(1-((9H-Purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
Synonyms: (S)-2-(1-((9H-Purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one;CAL-101;(S)-2-(1-(9H-Purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one;4(3H)​-​Quinazolinone,5-​fluoro-​3-​phenyl-​2-​[(1S)​-​1-​(9H-​purin-​6-​ylamino)​propyl]​-;CAL101;CAL-101 (GS-1101);CAL-101 (Idelalisib, GS-1101);CAL-101 (Idelalisib, GS-1101, CAL 101, CAL101);Idelalisib;Idelalisib （CAL101）;Idelalisib (CAL-101, GS-1101);Idelalisib-D5;GS1101;GS-1101
SMILES: O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)CC)=NC5=C1C(F)=CC=C5
Formula: C22H18N7OF
M.Wt: 415.42302
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Idelalisib (CAL-101) is a highly selective and potent p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
In Vivo: A significant reduction is observed in the CD11b+Ly6G+ neutrophils from brain homogenates of bothp110δD910A/D910A mice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice[3].
In Vitro: Idelalisib (CAL-101) is a highly selective and potent p110δ inhibitor (EC50=8 nM). Greater selectivity (400- to 4000-fold) is seen against related kinases C2β, hVPS34, DNA-PK, and mTOR, whereas no activity is observed against a panel of 402 diverse kinases at 10 μM. CAL-101 reduces PDGF-induced pAkt by only 25% at 10 μM. Idelalisib (CAL-101) inhibits LPA-induced pAkt with an EC50 of 1.9 μM. Idelalisib (CAL-101) blocks FcϵRI p110δ-mediated CD63 expression with an EC50 of 8 nM, whereas formyl-methionyl-leucyl-phenylalanine activation of p110γ is inhibited with an EC50 of 3 μM. Thus, in cell-based assays, CAL-101 has 240- to 2500-fold selectivity for p110δ over the other class I PI3K isoforms[1]. CAL-101Idelalisib (CAL-101)-induced apoptosis of chronic lymphocytic leukemia (CLL) cells is significant compare with vehicle treatment alone (P<0.001). Idelalisib (CAL-101) induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7238 Gedatolisib(PKI-587) PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively.
DC5072 Duvelisib (IPI-145, INK1197) Duvelisib (IPI-145) is a selective inhibitor of the p110δ isoform, exhibiting IC50 values of 2.5 nM, 27.4 nM, 85 nM, and 1602 nM for p110δ, p110γ, p110β, and p110α, respectively, highlighting its specificity and potency.
DC5068 Idelalisib (CAL-101,GS-1101) CAL-101 is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
DC5154 BKM120 (NVP-BKM120, Buparlisib) BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.
DC8760 Acalisib Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.
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