GSK2334470

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MedKoo CAT#: 406156

CAS#: 1227911-45-6

Description: GSK2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM), which does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. GSK2334470 also inhibited T-loop phosphorylation and activation of Akt. GSK2334470 will be a useful tool for delineating the roles of PDK1 in biological processes.


Price and Availability

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Pricing updated 2020-07-15. Prices are subject to change without notice.

GSK2334470 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406156
Name: GSK2334470
CAS#: 1227911-45-6
Chemical Formula: C25H34N8O
Exact Mass: 462.28556
Molecular Weight: 462.59
Elemental Analysis: C, 64.91; H, 7.41; N, 24.22; O, 3.46


Synonym: GSK2334470; GSK 2334470; GSK-2334470

IUPAC/Chemical Name: (3S,6R)-1-(6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl)-N-cyclohexyl-6-methylpiperidine-3-carboxamide

InChi Key: QLPHOXTXAKOFMU-WBVHZDCISA-N

InChi Code: InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1

SMILES Code: O=C([C@@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[C@H](C)CC1)NC5CCCCC5


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Najafov A, Shpiro N, Alessi DR. Akt is efficiently activated by PIF-pocket- and PtdIns(3,4,5)P3-dependent mechanisms leading to resistance to PDK1 inhibitors. Biochem J. 2012 Dec 1;448(2):285-95. doi: 10.1042/BJ20121287. PubMed PMID: 23030823.

2: Raimondi C, Chikh A, Wheeler AP, Maffucci T, Falasca M. A novel regulatory mechanism links PLCγ1 to PDK1. J Cell Sci. 2012 Jul 1;125(Pt 13):3153-63. doi: 10.1242/jcs.100511. Epub 2012 Mar 27. PubMed PMID: 22454520; PubMed Central PMCID: PMC3434861.

3: Knight ZA. For a PDK1 inhibitor, the substrate matters. Biochem J. 2011 Jan 15;433(2):e1-2. doi: 10.1042/BJ20102038. PubMed PMID: 21175429.

4: Najafov A, Sommer EM, Axten JM, Deyoung MP, Alessi DR. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J. 2011 Jan 15;433(2):357-69. doi: 10.1042/BJ20101732. PubMed PMID: 21087210.