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MedKoo product information:

  

 KP372-1

   

Description of KP372-1: KP372-1 is a synthetic small molecule AKT inhibitor. KP372-1 is consisted of two isomers:  KP372-1A and KP372-1B. KP372-1 showed activities to block signalling downstream of Akt in thyroid tumour cells, leading to inhibition of cell proliferation and increased apoptosis.  KP372-1 has also been shown to suppress cell proliferation and induce apoptosis in gliobastoma.

 

Current developer: 

   

MedKoo Code#:  401520

Name: KP372-1

CAS#:  329710-24-9

 

Synonym:   KP372-1

   

IUPAC/Chemical name: 

KP372-1A: 10H-indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one

KP372-1B: 6H-indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one

  

Chemical structure

Theoretical analysis

 

KP372-1A

 

KP372-1B

 

 

MedKoo Code#:  401520
Name: KP372-1
CAS#:  329710-24-9

Chemical Formula: C10H4N6O

Exact Mass: 224.04466

Molecular Weight: 224.17836

Elemental Analysis: C, 53.58; H, 1.80; N, 37.49; O, 7.14

 

 

Availability and price:

This agent is  available through  custom synthesis.

 

To inquire quotation and lead time or to ask questions, 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.

 

 

Information about this agent

 

 

 

References

1: Liu B, Wu JM, Li J, Liu JJ, Li WW, Li CY, Xu HL, Bao JK. Polygonatum cyrtonema lectin induces murine fibrosarcoma L929 cell apoptosis and autophagy via blocking Ras-Raf and PI3K-Akt signaling pathways. Biochimie. 2010 Dec;92(12):1934-8. Epub 2010 Aug 14. PubMed PMID: 20713122.

2: Shao H, Yi XM, Wells A. Epidermal growth factor protects fibroblasts from apoptosis via PI3 kinase and Rac signaling pathways. Wound Repair Regen. 2008 Jul-Aug;16(4):551-8. PubMed PMID: 18638274; PubMed Central PMCID: PMC2547354.

3: Xi RG, Huang J, Li D, Wang XB, Wu LJ. Roles of PI3-K/Akt pathways in nanoparticle realgar powders-induced apoptosis in U937 cells. Acta Pharmacol Sin. 2008 Mar;29(3):355-63. PubMed PMID: 18298901.

4: Li D, Cui Q, Chen SG, Wu LJ, Tashiro S, Onodera S, Ikejima T. Inactivation of ras and changes of mitochondrial membrane potential contribute to oridonin-induced autophagy in a431 cells. J Pharmacol Sci. 2007 Sep;105(1):22-33. PubMed PMID: 17895587.

5: Zeng Z, Samudio IJ, Zhang W, Estrov Z, Pelicano H, Harris D, Frolova O, Hail N Jr, Chen W, Kornblau SM, Huang P, Lu Y, Mills GB, Andreeff M, Konopleva M. Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Res. 2006 Apr 1;66(7):3737-46. PubMed PMID: 16585200.

6: Koul D, Shen R, Bergh S, Sheng X, Shishodia S, Lafortune TA, Lu Y, de Groot JF, Mills GB, Yung WK. Inhibition of Akt survival pathway by a small-molecule inhibitor in human glioblastoma. Mol Cancer Ther. 2006 Mar;5(3):637-44. PubMed PMID: 16546978.

7: Mandal M, Younes M, Swan EA, Jasser SA, Doan D, Yigitbasi O, McMurphey A, Ludwick J, El-Naggar AK, Bucana C, Mills GB, Myers JN. The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck. Oral Oncol. 2006 Apr;42(4):430-9. Epub 2006 Jan 27. PubMed PMID: 16442835; PubMed Central PMCID: PMC1414640.

8: Mandal M, Kim S, Younes MN, Jasser SA, El-Naggar AK, Mills GB, Myers JN. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. Br J Cancer. 2005 May 23;92(10):1899-905. PubMed PMID: 15870708; PubMed Central PMCID: PMC2361761.

  

 

 

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