PIK-90 free base · Synonyms: PIK 90 · PIK90

PIK-90 is a DNA-PK and PI3K inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K DNA-PK

Research area Cancer

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Data Sheet SDS COA

PIK-90 structure

CAS No.: 677338-12-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 498.00	BP-02509-500mg	In stock	Get quote
1 g	USD 985.00	BP-02509-1g	In stock	Get quote
2 g	USD 1,685.00	BP-02509-2g	In stock	Get quote
5 g	Inquire	BP-02509-5g	In stock	Inquire

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Description

PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.

Biological activity

PIK-90 is a novel and potent PI3K inhibitor with IC50 values of 11 nM, 350 nM, 18 nM and 58 nM for p110α, p110β, p110γ and p110δ respectively. Phosphoinositide 3-kinases (PI3Ks) are among the most frequently activated signaling pathways in cancer. Inhibition with p110alpha inhibitor PIK-90 resulted in a significant reduction of chemotaxis and actin polymerization to CXCL12 and reduced migration beneath MSC (pseudoemperipolesis). In suspension and MSC cocultures, PIK-90 was potent inducers of CLL cell apoptosis.

Identifiers

SMILES: COC1=C(OC)C2=C(C=C1)C1=NCCN1C(NC(=O)C1=CC=CN=C1)=N2
InChIKey: ZJAVHOMVDCMAMF-UHFFFAOYSA-N

Specifications

MW (average): 351.3593
Formula: C₁₈H₁₇N₅O₃
CAS No.: 677338-12-4
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C 3 years; 4°C 2 years. In solvent -20°C 1 year

Solubility

Soluble in DMSO; HCl

In vitro: 1 M HCl : 100 mg/mL DMSO : 6.67 mg/mL

Documents

References

[1].Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47.

[2].Niedermeier M, et al. Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach. Blood. 2009 May 28;113(22):5549-57.

[3].Cheng CK, et al. Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12722-7.

Same target

Search PI3K

Same research area

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