CAL-101 (GS-1101)

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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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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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