Cat. No.: HY-13026

Idelalisib

(Synonyms: CAL-101; GS-1101)

57 Cited Publications

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Based on 57 publication(s) in Google Scholar

Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC₅₀ of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

For research use only. We do not sell to patients.

Purity: 99.94%
CAS No.: 870281-82-6
Formula: C₂₂H₁₈FN₇O
Molecular Weight:415.42

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Idelalisib Chemical Structure

CAS No.: 870281-82-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (57)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

p110δ

2.5 nM (IC₅₀)

p110γ

89 nM (IC₅₀)

p110β

565 nM (IC₅₀)

p110α

820 nM (IC₅₀)

hVps34

978 nM (IC₅₀)

DNA-PK

6729 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A498	GI₅₀	1.1 μM Compound: Idelalisib	Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
A549	IC₅₀	0.33 μM Compound: CAL-101	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
B-cell	IC₅₀	0.0061 μM Compound: 74, GS-1101, CAL-101	Inhibition of PI3Kdelta in B-cells by proliferation assay Inhibition of PI3Kdelta in B-cells by proliferation assay	[PMID: 22924688]
Bel-7402	IC₅₀	66.23 μM Compound: CAL-101	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
CAKI-1	GI₅₀	20.5 μM Compound: Idelalisib	Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
CCRF-CEM	GI₅₀	22.3 μM Compound: Idelalisib	Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
DOHH-2	IC₅₀	0.86 μM Compound: Idelalisib	Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 35247756]
EOL1	IC₅₀	>50 μM Compound: CAL-101	Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth	[PMID: 36706844]
HCC 2998	GI₅₀	38.5 μM Compound: Idelalisib	Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HCT-116	IC₅₀	>10 μM Compound: Idelalisib	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 31434616]
HCT-116	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
HCT-116	IC₅₀	2.96 μM Compound: 1	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
HEK293	IC₅₀	>20 μM Compound: Idelalisib	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]
HeLa	IC₅₀	0.15 μM Compound: CAL-101	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	10.1039/C5MD00364D
Hep 3B2	IC₅₀	77.55 μM Compound: CAL-101	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
HepG2	IC₅₀	0.92 μM Compound: CAL-101	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
HepG2	IC₅₀	89.5 μM Compound: CAL-101	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
HL-60	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human HL-60 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
HL-60	IC₅₀	0.48 μM Compound: CAL-101	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth	[PMID: 36706844]
HOP-62	GI₅₀	>100 μM Compound: Idelalisib	Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HOP-92	GI₅₀	14.1 μM Compound: Idelalisib	Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Hs-578T	GI₅₀	6 μM Compound: Idelalisib	Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HT	IC₅₀	>10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
HUVEC	IC₅₀	38.22 μM Compound: 1	Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
IGROV-1	GI₅₀	4.8 μM Compound: Idelalisib	Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
JeKo-1	IC₅₀	0.12 μM Compound: Idelalisib	Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
Jurkat	IC₅₀	7.9 μM Compound: Idelalisib	Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
KARPAS-422	GI₅₀	0.68 μM Compound: CAL-101	Growth inhibition of human KARPAS422 cells by CCK8 assay Growth inhibition of human KARPAS422 cells by CCK8 assay	[PMID: 28835805]
KARPAS-422	IC₅₀	8.1 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
KG-1	IC₅₀	15.2 μM Compound: CAL-101	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth Antiproliferative activity against human KG-1 cells assessed as inhibition of cell growth	[PMID: 36706844]
KM12	GI₅₀	1.2 μM Compound: Idelalisib	Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
KM12	IC₅₀	0.96 μM Compound: 1	Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
L02	IC₅₀	>20 μM Compound: Idelalisib	Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]
LOUCY	IC₅₀	8.4 μM Compound: Idelalisib	Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
LOX IMVI	GI₅₀	33.5 μM Compound: Idelalisib	Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
M14	GI₅₀	37.8 μM Compound: Idelalisib	Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
MCF7	IC₅₀	>10 μM Compound: Idelalisib	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31434616]
MCF7	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
MCF7	IC₅₀	0.78 μM Compound: CAL-101	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
MDA-MB-231	GI₅₀	42.3 μM Compound: Idelalisib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
MOLM-13	GI₅₀	1.7 μM Compound: 1; CAL-101	Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLM-13	IC₅₀	3.66 μM Compound: Idelalisib	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 48 to 72 hrs by MTT assay	[PMID: 38577724]
MOLM-14	GI₅₀	6.4 μM Compound: 1; CAL-101	Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLM-14	IC₅₀	3.6 μM Compound: Idelalisib	Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
MOLM-16	IC₅₀	13.3 μM Compound: CAL-101	Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth Antiproliferative activity against human MOLM16 cells assessed as inhibition of cell growth	[PMID: 36706844]
MOLT-4	IC₅₀	>10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
MOLT-4	IC₅₀	10.6 μM Compound: Idelalisib	Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
MRC5	IC₅₀	>100 μM Compound: 1; 6c	Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34332211]
MV4-11	GI₅₀	>10 μM Compound: 1; CAL-101	Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MV4-11	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
MV4-11	IC₅₀	14.4 μM Compound: Idelalisib	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 48 to 72 hrs by MTT assay	[PMID: 38577724]
MV4-11	IC₅₀	4.3 μM Compound: CAL-101	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth	[PMID: 36706844]
MV4-11	IC₅₀	6.3 μM Compound: Idelalisib	Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
NALM-6	GI₅₀	>10 μM Compound: 1; CAL-101	Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
NAMALVA	IC₅₀	>10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
NCM460	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human NCM460 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCM460 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
Neutrophil	IC₅₀	0.07 μM Compound: Idelalisib	Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b	[PMID: 27142697]
Neutrophil	IC₅₀	0.07 μM Compound: Idelalisib	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins	[PMID: 28648460]
Neutrophil	IC₅₀	0.1 μM Compound: CAL-101	Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal	[PMID: 27525452]
Neutrophil	IC₅₀	0.3 μM Compound: CAL-101	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction	[PMID: 27525452]
Neutrophil	IC₅₀	0.3 μM Compound: Idelalisib	Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate	[PMID: 27142697]
Neutrophil	IC₅₀	0.3 μM Compound: Idelalisib	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide	[PMID: 28648460]
OCI-Ly10	IC₅₀	>10 μM Compound: Idelalisib	Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
OCI-Ly10	IC₅₀	31.9 nM Compound: 1; CAL-101	Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
OCI-Ly3	IC₅₀	5.2 μM Compound: Idelalisib	Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
OVCAR-3	GI₅₀	17.7 μM Compound: Idelalisib	Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
PF-382	GI₅₀	>10 μM Compound: 1; CAL-101	Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
Pfeiffer	GI₅₀	0.74 μM Compound: CAL-101	Growth inhibition of human Pfeiffer cells by CCK8 assay Growth inhibition of human Pfeiffer cells by CCK8 assay	[PMID: 28835805]
Pfeiffer	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by MTT assay Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
Pfeiffer	IC₅₀	6.8 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
Raji	IC₅₀	>10 μM Compound: Idelalisib	Antiproliferative activity against human Raji cells by MTT assay Antiproliferative activity against human Raji cells by MTT assay	[PMID: 31434616]
Raji	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human Raji cells incubated for 72 hrs by MTT assay Antiproliferative activity against human Raji cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
Raji	IC₅₀	9.95 nM Compound: Idelalisib	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 28325601]
Raji	IC₅₀	9.95 μM Compound: 1; CAL-101	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 29534936]
Ramos	IC₅₀	>10 nM Compound: Idelalisib	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 28325601]
Ramos	IC₅₀	>10 μM Compound: 1; CAL-101	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 29534936]
Ramos	IC₅₀	>10 μM Compound: Idelalisib	Antiproliferative activity against human Ramos cells by MTT assay Antiproliferative activity against human Ramos cells by MTT assay	[PMID: 31434616]
Ramos	IC₅₀	>10 μM Compound: CAL-101	Antiproliferative activity against human Ramos cells incubated for 72 hrs by MTT assay Antiproliferative activity against human Ramos cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
Ramos	IC₅₀	0.004 μM Compound: 1; CAL-101, GS-1101	Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins	[PMID: 31033293]
RAW264.7	IC₅₀	0.337 μM Compound: 1; CAL-101, GS-1101	Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins	[PMID: 31033293]
RPMI-8226	IC₅₀	5.49 μM Compound: 1; CAL-101	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 29534936]
RXF 393	GI₅₀	1.4 μM Compound: Idelalisib	Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Sf21	IC₅₀	0.002 μM Compound: 1; CAL-101, GS-1101	Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po	[PMID: 31033293]
Sf21	IC₅₀	0.293 μM Compound: 1; CAL-101, GS-1101	Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol	[PMID: 31033293]
Sf21	IC₅₀	154 nM Compound: 1	Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay	[PMID: 30878826]
Sf21	IC₅₀	3807 nM Compound: Idelalisib	Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells	[PMID: 30530193]
SNB-75	GI₅₀	1.2 μM Compound: Idelalisib	Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
SUD4	IC₅₀	1.6 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-1	IC₅₀	>10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL10	IC₅₀	>10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-6	GI₅₀	0.02 μM Compound: 1	Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30996859]
SU-DHL-6	GI₅₀	0.042 μM Compound: CAL-101; 1	Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay	[PMID: 29601991]
SU-DHL-6	GI₅₀	124 nM Compound: 1	Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 30878826]
SU-DHL-6	GI₅₀	34 nM Compound: Idelalisib	Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32078865]
SU-DHL-6	IC₅₀	0.033 μM Compound: Idelalisib	Antiproliferative activity against human SUDHL6 cells by MTT assay Antiproliferative activity against human SUDHL6 cells by MTT assay	[PMID: 31434616]
SU-DHL-6	IC₅₀	0.053 μM Compound: 1	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
SU-DHL-6	IC₅₀	0.1 μM Compound: CAL-101	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by MTT assay	[PMID: 38367493]
SU-DHL-6	IC₅₀	0.12 μM Compound: Idelalisib	Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
SU-DHL-6	IC₅₀	0.65 μM Compound: 1; CAL-101	Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay	[PMID: 29534936]
SU-DHL-6	IC₅₀	117.6 nM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-6	IC₅₀	22.5 nM Compound: 1; CAL-101	Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
T47D	GI₅₀	5.2 μM Compound: Idelalisib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
T47D	IC₅₀	0.51 μM Compound: 1	Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
TMD8	IC₅₀	7.3 nM Compound: 1; CAL-101	Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
TMD8	IC₅₀	795 nM Compound: GS-1101; CAL-101	Antiproliferative activity against human TMD8 cells Antiproliferative activity against human TMD8 cells	[PMID: 30975623]
U-251	GI₅₀	53.2 μM Compound: Idelalisib	Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Vero	IC₅₀	>20 μM Compound: Idelalisib	Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]

In Vitro

Idelalisib (CAL-101; GS-1101) 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 Fc?RI 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

A significant reduction is observed in the CD11b⁺Ly6G⁺ neutrophils from brain homogenates of bothp110δ^D910A/D910A mice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 870281-82-6
Appearance Solid
Molecular Weight 415.42
Formula C₂₂H₁₈FN₇O
Color White to off-white
SMILES

O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)CC)=NC5=C1C(F)=CC=C5
Synonyms

CAL-101; GS-1101
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (57)

All WBCell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

Cancer Cell

Evolutionary states and trajectories characterized by distinct pathways stratify patients with ovarian high grade serous carcinoma. [Abstract]

2023 Jun 12;41(6):1103-1117.e12. PMID: 37207655
Mol Cancer

Overexpression of wild type RRAS2, without oncogenic mutations, drives chronic lymphocytic leukemia. [Abstract]

2022 Feb 4;21(1):35. PMID: 35120522
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Exp Hematol Oncol

Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]

2016 Jul 29:5:22. PMID: 27478685
Leukemia

The WHIM-like CXCR4(S338X) somatic mutation activates AKT and ERK, and promotes resistance to ibrutinib and other agents used in the treatment of Waldenstrom's Macroglobulinemia. [Abstract]

2015 Jan;29(1):169-76. PMID: 24912431
Clin Cancer Res

Synergistic Targeting of the Regulatory and Catalytic Subunits of PI3Kδ in Mature B-cell Malignancies. [Abstract]

2018 Mar 1;24(5):1103-1113. PMID: 29246942
Cancer Lett

PI3K inhibitor idelalisib enhances the anti-tumor effects of CDK4/6 inhibitor palbociclib via PLK1 in B-cell lymphoma. [Abstract]

2024 May 28:216996. PMID: 38815797
Cell Death Dis

Selective PI3Kδ inhibitor TYM-3-98 suppresses AKT/mTOR/SREBP1-mediated lipogenesis and promotes ferroptosis in KRAS-mutant colorectal cancer. [Abstract]

2024 Jul 3;15(7):474. PMID: 38956060
Phytomedicine

CBX5 loss drives Pl3Kδ inhibitor resistance in mantle cell lymphoma and propolis restores sensitivity by inducing CBX5-mediated ferroptosis. [Abstract]

2025 May 27:143:156911. PMID: 40466505
EMBO Mol Med

A novel model of glioblastoma recurrence to identify therapeutic vulnerabilities. [Abstract]

2025 Jun;17(6):1325-1354. PMID: 40295888
NPJ Precis Oncol

Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]

2025 Nov 21;9(1):373. PMID: 41272086
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Cell Rep

Divergent Roles of PI3K Isoforms in PTEN-Deficient Glioblastomas. [Abstract]

2020 Sep 29;32(13):108196. PMID: 32997991
Br J Cancer

Transcriptome analysis of newly established carboplatin-resistant ovarian cancer cell model reveals genes shared by drug resistance and drug-induced EMT. [Abstract]

2023 Mar;128(7):1344-1359. PMID: 36717670
J Med Chem

Discovery of ( S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1 H-pyrazolo[3,4- d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3 H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease. [Abstract]

2020 Nov 25;63(22):13973-13993. PMID: 33180507
Cell Biosci

Inhibition of PI3 kinase isoform p110α suppresses neuroblastoma growth and induces the reduction of Anaplastic Lymphoma Kinase. [Abstract]

2022 Dec 30;12(1):210. PMID: 36585695
EMBO Rep

Class IA PI3Ks regulate subcellular and functional dynamics of IDO1. [Abstract]

2020 Dec 3;21(12):e49756. PMID: 33159421
Biochem Pharmacol

EP4 receptor agonist L-902688 augments cytotoxic activities of ibrutinib, idelalisib, and venetoclax against chronic lymphocytic leukemia cells. [Abstract]

2021 Jan;183:114352. PMID: 33278351
Life Sci

TYM-3-98, a novel selective inhibitor of PI3Kδ, demonstrates promising preclinical antitumor activity in B-cell lymphomas. [Abstract]

2024 Jun 15:347:122662. PMID: 38670450
Int J Mol Sci

The PI3Kδ Inhibitor Idelalisib Diminishes Platelet Function and Shows Antithrombotic Potential. [Abstract]

2021 Mar 24;22(7):3304. PMID: 33804911
Int Immunopharmacol

Idelalisib modulates CD4+ T cell responses to mitigate rejection of allografts in mice. [Abstract]

2025 Sep 23:162:115155. PMID: 40602262
RSC Adv

Integrative machine learning-guided in silico and in vitro approach reveals selective small molecule inhibitors targeting mutant IDH1. [Abstract]

2025 Dec 18;15(59):50944-50962. PMID: 41426059
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Cell Rep Methods

Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]

2026 Jun 15;6(6):101339. PMID: 42134319
Mol Oncol

The PI3Kδ inhibitor roginolisib (IOA-244) preserves T-cell function and activity. [Abstract]

2026 Jan 22. PMID: 41568714
J Biol Chem

The mTOR inhibitor manassantin B reveals a crucial role of mTORC2 signaling in Epstein-Barr virus reactivation. [Abstract]

2020 May 22;295(21):7431-7441. PMID: 32312752
Br J Haematol

Evaluation of the PIK3 pathway in peripheral T-cell lymphoma and NK/T-cell lymphoma. [Abstract]

2020 May;189(4):731-744. PMID: 32004387
Br J Haematol

The BCL2 antagonist ABT-199 triggers apoptosis, and augments ibrutinib and idelalisib mediated cytotoxicity in CXCR4 Wild-type and CXCR4 WHIM mutated Waldenstrom macroglobulinaemia cells. [Abstract]

2015 Jul;170(1):134-8. PMID: 25582069

Idelalisib purchased from MedChemExpress. Usage Cited in: Br J Haematol. 2015 Jul;170(1):134-8. [Abstract]

Treatment of CXCR4^WT and CXCR4^S338X BCWM.1 and MWCL-1 cells with PCI-32765 or Idelalisib induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following PCI-32765 (IB), Idelalisib (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).
Eur J Immunol

Anti-SARS-CoV-2 Spike IgA2 Induces Inflammation by Human Macrophages. [Abstract]

2025 Oct;55(10):e70068. PMID: 41054024
Cell Signal

BTK-independent regulation of calcium signalling downstream of the B-cell receptor in malignant B-cells. [Abstract]

2022 Aug:96:110358. PMID: 35597428
Med Oncol

Novel PI3Kδ inhibitor exerts antitumor activity in Burkitt lymphoma by inducing ROS-dependent apoptosis. [Abstract]

2025 Jun 21;42(7):277. PMID: 40544227
Cancer Res Commun

Cooperative Roles of Class IA PI3K Isoforms in Translocation-Related Sarcoma Cell Survival and Proliferation. [Abstract]

2026 Apr 1;6(4):976-993. PMID: 41916029
Hum Cell

Hypothermic machine perfusion reduces donation after circulatory death liver ischemia-reperfusion injury through the SERPINA3-mediated PI3Kδ/Akt pathway. [Abstract]

2024 Mar;37(2):420-434. PMID: 38133876
Cancer Med

Modulation of intracellular kinase signaling to improve TIL stemness and function for adoptive cell therapy. [Abstract]

2023 Feb;12(3):3313-3327. PMID: 36028997
Am J Cancer Res

A long-lasting PI3Kδ inhibitor zandelisib forms a water-shielded hydrogen bond with p110δ and demonstrates sustained inhibitory effects. [Abstract]

2025 May 15;15(5):2097-2110. PMID: 40520883
PLoS One

Exosomes from human umbilical cord mesenchymal stem cells promote the growth of human hair dermal papilla cells. [Abstract]

2025 Apr 30;20(4):e0320154. PMID: 40305498
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Mol Cell Neurosci

GPR3 accelerates neurite outgrowth and neuronal polarity formation via PI3 kinase-mediating signaling pathway in cultured primary neurons. [Abstract]

2022 Jan:118:103691. PMID: 34871769
Eur J Haematol

Interferon gamma regulates a complex pro-survival signal network in chronic lymphocytic leukemia. [Abstract]

2023 Apr;110(4):435-443. PMID: 36576398
Leuk Res

PI3K/AKT confers intrinsic and acquired resistance to pirtobrutinib in chronic lymphocytic leukemia. [Abstract]

2024 Jul 7:144:107548. PMID: 39018782
J Chemother

Idelalisib induces apoptosis in the lymphoid tissues and impairs lung function in mice. [Abstract]

2020 Apr;32(2):88-97. PMID: 31884896
Res Sq

2025 Aug 31.
Patent

US20240325538A1.
Patent

US20240238271A1.
bioRxiv

Tumor microenvironment immunomodulation by nanoformulated TLR 7/8 agonist and PI3k delta inhibitor enhances therapeutic benefits of radiotherapy. [Abstract]

2024 Mar 13:2024.03.09.584084. PMID: 38559220
Patent

US20230226111A1.
Patent

US20230058557A1.
University of Rijeka

2023.
Patent

US20200199683A1
Charles University

2019 Jun.
Oncotarget

Simultaneous inhibition of Vps34 kinase would enhance PI3Kδ inhibitor cytotoxicity in the B-cell malignancies. [Abstract]

2016 Aug 16;7(33):53515-53525. PMID: 27447747

Idelalisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]

PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.
Patent

US20160222465A1.
Oncotarget

Characterization of selective and potent PI3Kδ inhibitor (PI3KDIN- 015) for B-Cell malignances. [Abstract]

2016 May 31;7(22):32641-51. PMID: 27081697

Idelalisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]

The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC₅₀ of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.
Universität Würzburg

2016 April 27.
Int J Physiol Pathophysiol Pharmacol

The PI3Kδ inhibitor idelalisib suppresses liver and lung cellular respiration. [Abstract]

2015 Dec 13;7(3):115-25. PMID: 26823960
Am J Dig Dis (Madison)

2015;2(2):95-99.
Patent

US20110306622A1.

Solvent & Solubility

In Vitro:

DMSO : ≥ 59.7 mg/mL (143.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4072 mL

12.0360 mL

24.0720 mL

5 mM

0.4814 mL

2.4072 mL

4.8144 mL

10 mM

0.2407 mL

1.2036 mL

2.4072 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 3.33 mg/mL (8.02 mM); Clear solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 1% CMC/0.5% Tween-80 in Saline water

Solubility: 10 mg/mL (24.07 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

MTT assays are performed to determine cytotoxicity. Briefly, 1×10⁵ cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Idelalisib (CAL-101) (0.1 μM, 1 μM, 5 μM, 10 μM), 25 μM LY294002, or vehicle control. MTT reagent is then added. DMSO is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. At least 10,000 cells are counted for each sample. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100 μM Z-VAD. Experiments examining survival signals include the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture is done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice^[3]
For Idelalisib (CAL-101) treatment, wild-type C57BL/6 mice are administered either 40 mg/kg Idelalisib (CAL-101) or vehicle DMSO, by 25 μL infusion into the femoral vein, 15 min before I/R (pre-treatment), or 3 and 6 h after initiation of reperfusion (post-treatment). Controls and animals treated with Idelalisib (CAL-101) underwent cerebral blood flow (CBF) measurements using a laser Doppler perfusion monitor. The CBF measurements obtained immediately before and after MCAO and again at 3 h after reperfusion showed an ~90-95% reduction in the blood flow to the MCAO infarct region, which does not differ between groups.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lannutti BJ, et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood, 2011, 117(2), 591-594. [Content Brief]

[2]. Herman SE, et al. 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), 2078-2088. [Content Brief]

[3]. Low PC, et al. PI3Kδ inhibition reduces TNF secretion and neuroinflammation in a mouse cerebral stroke model. Nat Commun. 2014 Mar 14;5:3450. [Content Brief]

[4]. Cooney J, et al. Synergistic targeting of the regulatory and catalytic subunits of PI3Kδ in mature B cell malignancies. Clin Cancer Res. 2018 Mar 1;24(5):1103-1113. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4072 mL	12.0360 mL	24.0720 mL	60.1801 mL
	5 mM	0.4814 mL	2.4072 mL	4.8144 mL	12.0360 mL
	10 mM	0.2407 mL	1.2036 mL	2.4072 mL	6.0180 mL
	15 mM	0.1605 mL	0.8024 mL	1.6048 mL	4.0120 mL
	20 mM	0.1204 mL	0.6018 mL	1.2036 mL	3.0090 mL
	25 mM	0.0963 mL	0.4814 mL	0.9629 mL	2.4072 mL
	30 mM	0.0802 mL	0.4012 mL	0.8024 mL	2.0060 mL
	40 mM	0.0602 mL	0.3009 mL	0.6018 mL	1.5045 mL
	50 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2036 mL
	60 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0030 mL
	80 mM	0.0301 mL	0.1505 mL	0.3009 mL	0.7523 mL
	100 mM	0.0241 mL	0.1204 mL	0.2407 mL	0.6018 mL

Keywords

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Idelalisib

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Anti-COVID-19 Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Therapy Drug Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Withdrawn Drug Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Idelalisib

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (57)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Idelalisib Related Classifications

HY-13026 Related Classifications