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PI-103

Cayman Chemical Item Number 10009209

(CAS 371935-74-9)

PI-103 (CAS 371935-74-9)

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Description

The phosphatidylinositol 3-kinases (PI3K) family of enzymes is comprised of 15 members that are divided into 3 classes according to their structure, substrate specificity, and mode of regulation.1,2PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR. The IC50 values are 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.1 PI-103 exhibits antiproliferative activity against a panel of glioma cell lines in vitro at a concentration of 0.5 µM. It also inhibits growth of established human glioma tumor xenografts in vivo with no observable toxicity.3

1 Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 733-747 (2006).

2 Rückle, T., Schwarz, M.K., and Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'? Nat Rev Drug Discov 5 903-918 (2006).

3 Fan, Q., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9 341-349 (2006).

Formal Name 3-​[4-​(4-​morpholinyl)pyrido[3’,​2’:4,​5]furo[3,​2-​d]pyrimidin-​2-​yl]-​phenol
CAS Number 371935-74-9
Molecular Formula C19H16N4O3
Formula Weight 348.4
Formulation A crystalline solid
Purity ≥98%
λmax 221, 258, 285, 292 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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Oc1cccc(c1)​c1nc(N2CCOCC2)​c2oc3ncccc3c2n1

Background Reading

Fan, Q., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9 341-349 (2006).

Rückle, T., Schwarz, M.K., and Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'? Nat Rev Drug Discov 5 903-918 (2006).

Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 733-747 (2006).

PI-103 is available in the following screening libraries:

Size Price Quantity Subtotal
1 mg $23.00 $0.00
5 mg $92.00 $0.00
10 mg $138.00 $0.00
25 mg $259.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-05-25. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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