All AbMole products are for research use only, cannot be used for human consumption.
CAL-101 (Idelalisib; GS-1101) is a highly selective and potent p110δ small molecule inhibitor (half-maximal effective concentration [EC(50)] = 8nM). CAL-101 inhibits CLL cell chemotaxis toward CXCL12 and CXCL13 and migration beneath stromal cells (pseudoemperipolesis). CAL-101 (GS-1101) also down-regulates secretion of chemokines in stromal cocultures and after BCR triggering. CAL-101 reduces survival signals derived from the BCR or from nurse-like cells, and inhibits BCR- and chemokine-receptor-induced AKT and MAP kinase (ERK) activation. In stromal cocultures, CAL-101 sensitizes CLL cells toward bendamustine, fludarabine, and dexamethasone. CAL-101 (GS-1101) blocked constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis. CAL-101 displays a dual mechanism of action, directly decreasing cell survival while reducing interactions that retain CLL cells in protective tissue microenvironments.
Nat Commun. 2025 Jan 14;16(1):617.
Oncogenic role of RARG rearrangements in acute myeloid leukemia resembling acute promyelocytic leukemia
CAL-101 (Idelalisib) purchased from AbMole
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Source | Cancer Biol Med (2015). Figure 5. CAL-101 |
| Method | MTT assay | |
| Cell Lines | Z138, HBL-2, and Jeko-1 cells | |
| Concentrations | 20-100 μmol/L | |
| Incubation Time | 48 h | |
| Results | CAL-101 exhibited a time-dependent inhibitory effect on the viability of Z138, HBL-2, and Jeko-1 cells. CAL-101 and BTZ concentrations were fixed at 60 and 0.18 μmol/L, respectively |
| Cell Experiment | |
|---|---|
| Cell lines | Primary cortical neurons, astrocytes or microglia |
| Preparation method | Assaying TNF secretion For drug treatments, cells were incubated with IC87114, CAL-101 (AbMole, M1945) and LPS, glucose-free Locke’s buffer, or a combination thereof. For TNF surface delivery assay18, 32, TNF-converting enzyme inhibitor was added at the same time as LPS or included in the glucose-free Locke’s buffer. All inhibitors were reconstituted in Dimethyl sulfoxide (AbMole) with final concentrations <0.1% in assays. To determine the levels of secreted TNF, a commercial BD OptEIA TNF Elisa Set II kit was used to quantify cytokine concentration in samples according to the manufacturer’s instructions. |
| Concentrations | 0,1,5µM |
| Incubation time | 0~10h |
| Animal Experiment | |
|---|---|
| Animal models | wild-type (WT) or p110δD910A/D910A mice |
| Formulation | dimethylsulphoxide (DMSO) |
| Dosages | CAL-101 (40 mg k−1g i.v.) 15 min before ischaemia (CAL-101, Pre) or 3 h after reperfusion (CAL-101, Post) |
| Administration | i.v. |
| Molecular Weight | 415.42 |
| Formula | C22H18FN7O |
| CAS Number | 870281-82-6 |
| Solubility (25°C) | DMSO 59 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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|---|
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AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
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BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
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All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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