GSK2334470 | CAS#1227911-45-6 | MedKoo Biosciences

GSK2334470
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WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

GSK2334470

CAS# 1227911-45-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406156
Name: GSK2334470
CAS#: 1227911-45-6
Chemical Formula: C25H34N8O
Exact Mass: 462.29
Molecular Weight: 462.602
Elemental Analysis: C, 64.91; H, 7.41; N, 24.22; O, 3.46

Price and Availability

Size	Price	Availability
25mg	USD 450	2 Weeks
50mg	USD 750	2 Weeks
100mg	USD 1350	2 Weeks
200mg	USD 2350	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
In vitro activity:	Correctively, this data suggested that GSK-470 (GSK2334470) inhibited proliferation and induced apoptosis of MM (multiple myeloma) cells, and anti-myeloma effect of GSK-470 might correlate with the level of PTEN expression. Reference: Oncotarget. 2017 Jun 13;8(24):39185-39197. https://pubmed.ncbi.nlm.nih.gov/28402933/
In vivo activity:	Administration of the PDK1 inhibitor GSK2334470 (PDKi) effectively delayed melanomagenesis and metastasis in Braf(V600E)::Pten(-/-) mice. Pdk1(-/-) melanomas exhibit a marked decrease in the activity of AKT, P70S6K and PKC. Notably, PDKi was as effective in inhibiting AGC kinases and colony forming efficiency of melanoma with Pten wild-type (WT) genotypes. Reference: Oncogene. 2014 Aug 21;33(34):4330-9. https://pubmed.ncbi.nlm.nih.gov/24037523/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	20.0	43.23
	DMSO	52.1	112.55
	Ethanol	52.8	114.04
	Ethanol:PBS (pH 7.2) (1:1)	0.5	1.08

Preparing Stock Solutions

The following data is based on the product molecular weight 462.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Yang C, Huang X, Liu H, Xiao F, Wei J, You L, Qian W. PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242. Oncotarget. 2017 Jun 13;8(24):39185-39197. doi: 10.18632/oncotarget.16642. PMID: 28402933; PMCID: PMC5503605. 2. Scortegagna M, Ruller C, Feng Y, Lazova R, Kluger H, Li JL, De SK, Rickert R, Pellecchia M, Bosenberg M, Ronai ZA. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9. doi: 10.1038/onc.2013.383. Epub 2013 Sep 16. PMID: 24037523; PMCID: PMC3955742.
In vitro protocol:	1. Yang C, Huang X, Liu H, Xiao F, Wei J, You L, Qian W. PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242. Oncotarget. 2017 Jun 13;8(24):39185-39197. doi: 10.18632/oncotarget.16642. PMID: 28402933; PMCID: PMC5503605.
In vivo protocol:	1. Yang C, Huang X, Liu H, Xiao F, Wei J, You L, Qian W. PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242. Oncotarget. 2017 Jun 13;8(24):39185-39197. doi: 10.18632/oncotarget.16642. PMID: 28402933; PMCID: PMC5503605. 2. Scortegagna M, Ruller C, Feng Y, Lazova R, Kluger H, Li JL, De SK, Rickert R, Pellecchia M, Bosenberg M, Ronai ZA. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9. doi: 10.1038/onc.2013.383. Epub 2013 Sep 16. PMID: 24037523; PMCID: PMC3955742.

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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.

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