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CAL-101 (Idelalisib, GS-1101) PI3K inhibitor

Catalog No.A3005
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10mM (in 1mL DMSO)
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Evaluation Sample
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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Yaya Chu, Sanghoon Lee, et al. " Ibrutinib significantly inhibited Bruton’s tyrosine kinase (BTK) phosphorylation,in-vitro proliferation and enhanced overall survival in a preclinical Burkitt lymphoma (BL) model." OncoImmunology.11 Oct 2018.
2. Wensveen FM, Slinger E, et al. "Antigen-affinity controls pre-germinal centser B cell selection by promoting Mcl-1 induction through BAFF receptor signaling." Sci Rep. 2016 Oct 20;6:35673. PMID:27762293

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Chemical structure

CAL-101 (Idelalisib, GS-1101)

Related Biological Data

CAL-101 (Idelalisib, GS-1101)

Biological Activity

Description CAL-101 (Idelalisib, GS-1101) is a selective inhibitor of p110δ with IC50 of 2.5 nM.
Targets p110δ          
IC50 2.5 nM          


Cell experiment: [1]

Cell lines

CD19/CD5-positive CLL cells (> 90%)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

< 5 μM: dose-dependently inhibits the pro-survival effect of anti-IgM
= 5 μM, 24h: inhibits 2.6% activity of anti-IgM
> 5 μM, 72h: maximally reduces CLL cell viability


CAL-101 abrogated the pro-survival effect of anti-IgM in a dose-dependent fashion at lower dose levels (< 5 μM). CAL-101 treatment at concentrations of > 5 μM was maximally effective over the 72-hour time course in reducing CLL cell viability. At the 5 μM concentration, CAL-101 significantly decreased the mean ( SEM) pro-survival effect of anti-IgM to 92.7% ( 2.6%) after 24 hours.

Animal experiment : [2]

Animal models

NOD-SCID-γ-null (NSG) mice well-engrafted with de novo (n = 3) or relapsed (n = 1) childhood Ph-like ALL specimens with JAK2 mutations and/or CRLF2 alterations.

Dosage form

30 mg/kg/day, 3 days, oral gavage


CAL101 treatments demonstrated potent in vivo inhibition of relevant phosphoproteins, including phosphorylated (p) PI3K, mTOR, S6, and AktS473. Increased phosphorylation of other measured proteins was not observed, suggesting that proximal inhibition effectively abrogated aberrant PI3K pathway signal transduction with minimal compensatory signaling upregulation.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Hoellenriegel J, Meadows S A, Sivina M, et al. The phosphoinositide 3′-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood, 2011, 118(13): 3603-3612.

[2] Li Y, Ryan T, Vincent T, et al. In vivo efficacy of PI3K pathway signaling inhibition for Philadelphia chromosome-like acute lymphoblastic leukemia. Blood, 2013, 122(21): 2672-2672.

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Chemical Properties

Cas No. 870281-82-6 SDF Download SDF
Synonyms CAL-101,CAL101,Idelalisib,GS-1101,GS1101
Chemical Name 5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one
Canonical SMILES CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
Formula C22H18FN7O M.Wt 415.43
Solubility >20.8mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Research Update

2. The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood. 2011 Sep 29;118(13):3603-12. doi: 10.1182/blood-2011-05-352492. Epub 2011 Jul 29.
CAL-101 is a selective inhibitor of PI3Kδ that induces rapid lymph node shrinkage and a transient lymphocytosis in CLL cells. CAL-101 not only directly inhibits the pro-survival PI3K pathway but also disrupts CLL-microenvironment interactions, where it inhibits chemotaxis and migration of CLL cell, down-regulates BCR-induced chemokines secretion, reduces survival signals and suppresses ERK activation.
3. PI3Kδ inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma. Blood. 2012 Feb 23;119(8):1897-900. doi: 10.1182/blood-2011-10-386763. Epub 2011 Dec 30.
CAL-101, an oral inhibitor of PI3Kδ, inhibited AKT phosphorylation and stroma-induced Akt activation, reduced CCL5 production and dose-dependently induced apoptosis in HL cells. Moreover, addition of everolimu could enhance the anti-HL activity of CAL-101.
4. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011 Jan 13;117(2):591-4. doi: 10.1182/blood-2010-03-275305. Epub 2010 Oct 19.
CAL-101 is an inhibitor of p110δ that blocks phosphatidylinositol-3-kinase signaling in a wide range of B-cell malignancies leading to decreased phosphorylation of Akt and other downstream effectors, increased polu(ADP-ribose) polymerase and caspase cleavage and induced apoptosis.
5. Translating PI3K-Delta Inhibitors to the Clinic in Chronic Lymphocytic Leukemia: The Story of CAL-101 (GS1101). Am Soc Clin Oncol Educ Book. 2012;32:691-694. doi: 10.14694/EdBook_AM.2012.32.691.
CAL-101, a p110 delta inhibitor, has been developed fr the treatment of chronic lymphoid malignancies including CLL.


CAL-101 (Idelalisib, GS-1101), is a p110δ selective phosphatidylinositol-3-kinase inhibitor in a kinome-wide screen using purified enzymes and in cell-based PI3K isoform-specific assays. Phosphatidylinositol-3-kinase p110δ serves as a central integration point for signaling from cell surface receptors known to promote malignant B-cell proliferation and survival. CAL-101 can block constitutive phosphatidylinositol-3-kinase signaling, resulting in reduced phosphorylation of Akt and other downstream effect factors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis. These effects have been observed across a broad range of immature and mature B-cell malignancies. In addition, CAL-101 abrogated protection from spontaneous apoptosis induced by B cell–activating factors CD40L, TNF-α, and fibronectin.


Brian J. Lannutti, Sarah A. Meadows, Sarah E. M. Herman, Adam Kashishian, Bart Steiner, Amy J. Johnson, John C. Byrd, Jeffrey W. Tyner, Marc M. Loriaux, Mike Deininger, Brian J. Druker, Kamal D. Puri, Roger G. Ulrich, and Neill A. Giese. CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011; 117(2): 591 – 594.

Sarah E. M. Herman, Amber L. Gordon, Amy J. Wagner, Nyla A. Heerema, Weiqiang Zhao, Joseph M. Flynn, Jeffrey Jones, Leslie Andritsos, Kamal D. Puri, Brian J. Lannutti, Neill A. Giese, Xiaoli Zhang, Lai Wei, John C. Byrd,  Amy J. Johnson. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010; 116(12): 2078 – 88.