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PIK-75

Cayman Chemical Item Number 10009210

(CAS 372196-67-3)

PIK-75 (CAS 372196-67-3)

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Description

Phosphatidylinositol 3-kinase (PI3K) catalyzes the synthesis of the second messengers PtdIns-(3)-P, PtdIns-(3,4)-P2, and PtdIns-(3,4,5)-P3. The PI3K family of enzymes is comprised of 15 members that are divided into three classes according to their structure, substrate specificity, and mode of regulation.1 In the class I PI3Ks, p110α is the primary PI3K isoform required for insulin signaling in adipocytes and myotubes and is frequently mutated in primary tumors.2 Small molecule inhibitors of p110α are of interest in cancer treatment research. PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively.2 In adipocytes and myotubes, PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1.2

1 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).

2 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).

Formal Name 2-​methyl-​5-​nitro-​2-​[(6-​bromoimidazo[1,​2-​a]pyridin-​3-​yl)methylene]-​1-​methylhydrazide-​benzenesulfonic acid
CAS Number 372196-67-3
Molecular Formula C16H14BrN5O4S
Formula Weight 452.3
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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BrC1=CN2C(C=C1)​=NC(/C=N/N(S(C3=CC([N+]​([O-]​)​=O)​=CC=C3C)​(=O)​=O)​C)​=C2

Background Reading

Carracedo, A., and Pandolfi, P.P. The PTEN-PI3K pathway: Of feedbacks and cross-talks. Oncogene 27 5527-5541 (2008).

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).
Size Price Quantity Subtotal
1 mg $11.00 $0.00
5 mg $50.00 $0.00
10 mg $88.00 $0.00
25 mg $193.00 $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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