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MedKoo product information:
PIK-75
PIK-75 was developed as part of a PI 3-kinase drug
discovery program. PIK75 attenuates insulin stimulation of Akt/PKB in a
range of cell types at 100 nM. The compound has been reported to block
growth of a range of cell lines with an IC50 value in the region of 50
nM. In vivo studies have shown that PIK-75, administered at 50 mg/kg,
inhibited the growth of HeLa cell xenografts in mice models.
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MedKoo Code#: 202238
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Name: PIK-75
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CAS#: 372196-67-3
(PIK-75 free base); 372196-77-5 (PIK-75 hydrochloride)
Synonym:
PIK-75
IUPAC/Chemical name:
(E)-N'-((6-bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
hydrochloride
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Chemical structure
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Theoretical analysis
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PIK-75 (free base)
Chemical Formula: C16H14BrN5O4S
Exact Mass: 450.99499
Molecular Weight: 452.28
Elemental Analysis: C, 42.49; H, 3.12; Br,
17.67; N, 15.48; O, 14.15; S, 7.09
PIK-75 hydrochloride salt
Chemical Formula: C16H15BrClN5O4S
Molecular Weight: 488.74
Elemental Analysis: C, 39.32; H, 3.09; Br,
16.35; Cl, 7.25; N, 14.33; O, 13.09; S, 6.56.
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Availability and price:
PIK-75 (99%) is in
stock.
50 mg / $290.00
100 mg / $450.00
200 mg / $650.00
For quotation, question, and order, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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1: Dagia NM, Agarwal G, Kamath DV, Chetrapal-Kunwar
A, Gupte RD, Jadhav MG, Dadarkar SS, Trivedi J, Kulkarni-Almeida AA,
Kharas F, Fonseca LC, Kumar S, Bhonde MR. A preferential p110alpha/gamma
PI3K inhibitor attenuates experimental inflammation by suppressing the
production of proinflammatory mediators in a NF-kappaB-dependent manner.
Am J Physiol Cell Physiol. 2010 Apr;298(4):C929-41. Epub 2010 Jan 20.
PubMed PMID: 20089935.
2: Han M, Zhang JZ. Class I phospho-inositide-3-kinases (PI3Ks) isoform-specific
inhibition study by the combination of docking and molecular dynamics
simulation. J Chem Inf Model. 2010 Jan;50(1):136-45. PubMed PMID:
19928754.
3: Chaussade C, Cho K, Mawson C, Rewcastle GW, Shepherd PR. Functional
differences between two classes of oncogenic mutation in the PIK3CA
gene. Biochem Biophys Res Commun. 2009 Apr 17;381(4):577-81. Epub 2009
Feb 20. PubMed PMID: 19233141.
4: Kim JE, Shepherd PR, Chaussade C. Investigating the role of class-IA
PI 3-kinase isoforms in adipocyte differentiation. Biochem Biophys Res
Commun. 2009 Feb 20;379(4):830-4. Epub 2008 Dec 27. PubMed PMID:
19114029.
5: Zanella F, Rosado A, García B, Carnero A, Link W. Chemical genetic
analysis of FOXO nuclear-cytoplasmic shuttling by using image-based cell
screening. Chembiochem. 2008 Sep 22;9(14):2229-37. PubMed PMID:
18756565.
6: Hers I. Insulin-like growth factor-1 potentiates platelet activation
via the IRS/PI3Kalpha pathway. Blood. 2007 Dec 15;110(13):4243-52. Epub
2007 Sep 7. PubMed PMID: 17827393.
7: Kim S, Garcia A, Jackson SP, Kunapuli SP. Insulin-like growth
factor-1 regulates platelet activation through PI3-Kalpha isoform.
Blood. 2007 Dec 15;110(13):4206-13. Epub 2007 Sep 7. PubMed PMID:
17827385; PubMed Central PMCID: PMC2234779.
8: Chaussade C, Rewcastle GW, Kendall JD, Denny WA, Cho K, Grønning LM,
Chong ML, Anagnostou SH, Jackson SP, Daniele N, Shepherd PR. Evidence
for functional redundancy of class IA PI3K isoforms in insulin
signalling. Biochem J. 2007 Jun 15;404(3):449-58. PubMed PMID: 17362206;
PubMed Central PMCID: PMC1896275.
9. Hayakawa, M., Kawaguchi, K., Kaizawa, H.,
Koizumi, T., Ohishi, T., Yamano, M., Okada, M., Ohta, M., Tsukamoto, S.,
Raynaud, F. I., Parker, P., Workman, P. and Water?eld, M. D. (2007)
Synthesis and biological evaluation of sulfonylhydrazone- substituted
imidazo[1,2-a]pyridines as novel PI3 kinase p110a inhibitors.Bioorganic
Medicinal Chemistry 15, 5837-5844.
10 Chaussade, C., Rewcastle, G. W., Kendall, J. D.,
Denny, W. A., Cho, K., Gronning, L. M., Chong, M. L., Anagnostou, S. H.,
Jackson, S. P., Daniele, N. and Shepherd, P. R. (2007) Evidence for
functional redundancy of class IA PI3K isoforms in insulin
signalling.Biochem J 404, 449-5
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