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CAL-101 (GS-1101)
Cat No.
CEI-0117
Description
CAL-101 (GS-1101) can inhibit p110-delta with IC50 of 2.5 nM.
Alias
CAL101
CAS No.
870281-82-6
Molecular Weight
415.42
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
CAL101
Targets
p110-delta
Molecular Formula
C22H18FN7O
Chemical Name
(S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
Solubility
DMSO 83 mg/mL Water
In vitro
CAL-101, as a PI3K-delta selective inhibitor, can potently inhibit p110delta with IC50 of 2.5 nM and EC50 of 8nM. CAL-101 blocked constitutive phosphatidylinositol-3-kinase signaling as constitutive phosphatidylinositol-3-kinase pathway activation is p110delta-dependent. And the inhibition of PI3K by CAL-101 decrease phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis. For CLL, CAL-101 can promote apoptosis in primary CLL. CAL-101 cause cytotoxicity depend on caspase signaling. CAL-101 inhibits CLL cell chemotaxis toward CXCL12 and CXCL13 and migration beneath stromal cells (pseudoemperipolesis). CAL-101 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.
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