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CAL-101

Cat. No. M1945
CAL-101 Structure
Synonym:

GS-1101

Size Price Availability Quantity
10mg USD 65 In stock
50mg USD 170 In stock
100mg USD 260 In stock
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Quality Control
Biological Activity

CAL-101 (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.

Protocol
Cell Experiment
Cell lines Primary cortical neurons, astrocytes or microglia
Preparation method Assaying TNF secretion For drug treatments, cells were incubated with IC87114 (Symansis), CAL-101 (Active Biochem, #A-1138) and LPS, glucose-free Locke’s buffer (GD), 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 (GD). All inhibitors were reconstituted in dimethylsulphoxide (Sigma) with final concentrations <0.1% in assays. To determine the levels of secreted TNF, a commercial BD OptEIA TNF Elisa Set II (#558534) kit (BD Biosciences) 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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 415.42
Formula C22H18FN7O
CAS Number 870281-82-6
Purity 98.80%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

PI3Kδ inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma.
Meadows SA, et al. Blood. 2012 Feb 23;119(8):1897-900. PMID: 22210877.

The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia.
Hoellenriegel J, et al. Blood. 2011 Sep 29;118(13):3603-12. PMID: 21803855.

CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability.
Lannutti BJ, et al. Blood. 2011 Jan 13;117(2):591-4. PMID: 20959606.

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Keywords: CAL-101, GS-1101 supplier, PI3K, inhibitors

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