CAL-101 (GS-1101, Idelalisib)

Catalog No. A10172

CAL-101 (GS-1101,Idelalisib)是PI3K的同种型选择性抑制剂，可诱导慢性淋巴细胞性白血病（CLL）细胞凋亡。

Product Citations

Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
Yoshihiro Umezawa, .et al. Molecular mechanisms for enhancement of stromal cell-derived factor 1?Cinduced chemotaxis by platelet endothelial cell adhesion molecule 1 (PECAM-1), J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577

Technical details

Catalog Num	A10172
M. Wt	415.4
Formula	C22H18FN7O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	870281-82-6
Synonyms	CAL101
SMILES	CC[C@@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5

Biological Activity

CAL-101 (GS-1101,Idelalisib)是PI3K的同种型选择性抑制剂，可诱导慢性淋巴细胞性白血病（CLL）细胞凋亡。

Targets

Target	Value
p110δ	IC50: 2.5nM
p110γ	IC50: 89nM
p110β	IC50: 565nM
p110α	IC50: 820nM
hVps34	IC50: 978nM
C2β	IC50: >1μM
mTOR	IC50: >1μM
PIP5Kα	IC50: >1μM
PIP5Kβ	IC50: >1μM
DNA-PK	IC50: 6.729μM

Solubility *

In vitro (25°C)	DMSO	Warmed: 76 mg/mL (182.94 mM)
	Water	Insoluble
	Ethanol	21 mg/mL (50.55 mM)
In vivo	2% DMSO+20%PEG 300+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	24.07 mL	120.37 mL	240.73 mL
0.5 mM	4.81 mL	24.07 mL	48.15 mL
1 mM	2.41 mL	12.04 mL	24.07 mL
5 mM	0.48 mL	2.41 mL	4.81 mL

*The above data is based on the productmolecular weight 415.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.