PIK-90

PIK-90 is a potent PI3K inhibitor with potential anticancer activity.

Product information

CAS Number: 677338-12-4

Molecular Weight: 351.36

Formula: C18H17N5O3

Synonym:

PIK90

PIK 90

Chemical Name: N-(7, 8-dimethoxy-2, 3-dihydroimidazo[1, 2-c]quinazolin-5-yl)nicotinamide

Smiles: COC1=C2N=C(NC(=O)C3=CN=CC=C3)N3CCN=C3C2=CC=C1OC

InChiKey: ZJAVHOMVDCMAMF-UHFFFAOYSA-N

InChi: InChI=1S/C18H17N5O3/c1-25-13-6-5-12-14(15(13)26-2)21-18(23-9-8-20-16(12)23)22-17(24)11-4-3-7-19-10-11/h3-7,10H,8-9H2,1-2H3,(H,21,22,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 0.28 mg/mL(0.79 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PIK-90 shows distinct patterns of isoform selectivity to inhibit different subsets of four class I PI3K isoforms. In addition, PIK-90 completely inhibits the fMLP-stimulated phosphorylation of Akt and impairs polarity and chemotaxis in dHL60 cells. PIK-90 exhibits significantly antiproliferative activity by effectively blocking phosphorylation of Akt in six glioma cell lines varying in mutational status at PTEN or p53, including U87 MG, SF188, SF763, LN229, A1207 and LN-Z30 cells. Moreover, PIK-90 induces a modest G0G1 arrest at a concentration (0.5 μM) sufficient to inhibit phosphorylation of Akt substantially. In chronic lymphocytic leukemia (CLL) cells, PIK-90 inhibits chemotaxis to levels that are 57.8% of controls at 1 μM and 56.8% of controls at 10 μM. Consistently, PIK-90 inhibits pseudoemperipolesis to levels that are 74.2% PIK-90 of controls at 1 μM and 57.9% of controls at 10 μM. In addition, PIK-90 also leads to a significant reduction of CLL cell migration into the stromal cell layer and decreases CXCL12-induced actin polymerization.

In Vivo:

Immediately following insulin treatment, PIK-90 (10 mg/kg) completely protects animals from this insulin-stimulated decline in blood glucose.

References:

1. Niedermeier M, et al. Blood. 2009, 113(22), 5549-5557.
2. Fan QW, et al. Cancer Res. 2007, 67(17), 7960-7965.
3. Van Keymeulen A, et al. J Cell Biol. 2006, 174(3), 437-445.

Products are for research use only. Not for human use.