CAL-101 Inhibitor CAS No. 870281-82-6

Cat. No.	Name	Size	Price
KI0192	CAL-101	10 mg	$192
	CAL-101	50 mg	$360
	CAL-101	200 mg	$1200

Chemical Characteristic

Product Name	CAL-101
Synonyms	GS-1101
CAS No.	870281-82-6
Molecular Weight	415.42
Formula	C₂₂H₁₈FN₇O
Chemical Name	(S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one
Smiles	n1c(n(c(=O)c2c(cccc12)F)c1ccccc1)[C@H](CC)Nc1ncnc2[nH]cnc12
Chemical Structure
Documents	HPLC MS COA

Biological activities

CAL-101 is a potent and selective inhibitor of p110d with an IC50 of 2.5 nM. CAL-101 is 40- to 300-folds more selective for p110d relative to other dysregulation of the phosphatidylinositol-3-kinase (PI3K) class I enzymes, with IC50s of 820, 565, and 89 nM for p110a, p110b, and p110g, respectively. While, in related kinases C2b, hVPS34, DNA-PK, and mTOR, CAL-101 shows 400- to 4000-folds selectivity. CAL-101 reduces PDGF-induced pAkt by only 25% at 10 µM and inhibits LPA-induced pAkt with an EC50 of 1.9 µM. Besides, CAL-101 blocks FceRI (a high-affinity IgE receptor) p110d-mediated CD63 expression with an EC50 of 8 nM, whereas formyl-methionyl-leucyl-phenylalanine activation of p110d is inhibited with an EC50 of 3.0 µM. CAL-101 produces a concentration-dependent reduction in pAktS473, pAktT308, and the downstream target S6 with an EC50 of 0.1 to 1.0 µM. CAL-101 blocks constitutive oncogenic signaling, resulting in apoptosis, and inhibits survival signals provided by the microenvironment. ^[1] In addition, CAL-101 induces selective cytotoxicity in chronic lymphocytic leukemia (CLL) cells independent of IgVH mutational status or interphase cytogenetics. CAL-101 mediates cytotoxicity both by directly inhibiting CLL cell PI3K signaling and also antagonizing extrinsic activation of this pathway by CD40L, BAFF, TNF-a, fibronectin, and stromal cells.^[2] CAL-101 has broad antitumor activity against cancer cells of hematologic origin, and inhibits multiple myeloma (MM) cell growth even in the presence of interleukin-6 (IL-6), insulin-like growth factor-1 (IGF-1), or bone marrow stromal cells (BMSCs), associated with decreased phosphorylation of AKT and phosphorylated 70-kDa ribosomal S6 kinase (p70S6k). CAL-101 induces autophagy and synergistic cytotoxicity with bortezomib, and induction of phospho-Akt by bortezomib treatment is inhibited in the presence of CAL-101.^[3]

Protocols

CAL-101 is diluted in DMSO at a concentration of 10 mM . ^[1]

References

[1] Lannutti BJ, et al. CAL-101, a p110d selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011, 117(2): 591-594. [2] Herman SE, et al. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010, 116(12): 2078-2088. [3] Ikeda H, et al. PI3K/p110δ is a novel therapeutic target in multiple myeloma. Blood. 2010, 116(9): 1460-1468.

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