| Chemical & Physical Properties | |
|---|---|
| CAS Number | 1227911-45-6 |
| Catalog No. | 2A-2195382 |
| Chinese Name | GSK2334470 |
| Synonyms | CS-0917; QC-8425; GSK2334470 |
| Molecular Formula | C25H34N8O |
| Molecular Weight | 462.59 |
| Purity | ≥98 (HPLC) |
| Density | 1.3±0.1 g/cm3 |
| Appearance | powder |
| Water Solubility | DMSO: ≥10mg/mL |
| Storage Condition | 2-8°C |
| Application | GSK2334470 is a highly efficient and specific PDK1 inhibitor with an IC50 value of 10 nM. |
| PubChem ID | 329825237 |
| MDL Number | MFCD21608525 |
| SMILES | CNc1nc(cc(n1)-c2ccc3c(N)n[nH]c3c2)N4C[C@H](CC[C@H]4C)C(=O)NC5CCCCC5 |
| 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 |
| InChI Key | QLPHOXTXAKOFMU-WBVHZDCISA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| Hazard Symbols | transportation |
| MSDS | msds/197079_1_1227911_45_6.pdf |
| Bioactivity | GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM. Related Catalog Signaling Pathways >> PI3K/Akt/mTOR >> PDK-1 Research Areas >> Cancer Target IC50: 10 nM(PDK1)[1] In Vitro Small molecule GSK2334470 inhibits PDK1 with an IC50 of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. Addition of GSK2334470 ablates T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1). GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR, respectively, and induce higher G0-G1 ratio in LAN-1-MK than that in LAN-1 as well. PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines[2]. In Vivo The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten−/−mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1[3]. Cell Assay GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2]. Animal Admin Mice is dissolved in DMSO and then diluted with PBS or saline. BrafV600E::Pten−/− are generated as previously described. Cohorts of six animals per group are used in each experimental group. GSK2334470 is administered through IP injection (100 mg/kg) 3 times per week starting the same day of topical administration of 4-hydroxytamoxifen and ending at the time of mouse collection, based on earlier studies[3]. References [1]. Najafov A, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J.?2011 Jan 15;433(2):357-69. [2]. Qi L, et al. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int.?2015 Sep 29;15:91. [3]. Scortegagna M, et al. 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. Chemical & Physical Properties Density 1.3±0.1 g/cm3 Molecular Formula C25H34N8O Molecular Weight 462.591 Exact Mass 462.285553 PSA 132.30000 LogP 2.31 Appearance of Characters white to light brown Index of Refraction 1.667 InChIKey QLPHOXTXAKOFMU-WBVHZDCISA-N SMILES CNc1nc(-c2ccc3c(N)n[nH]c3c2)cc(N2CC(C(=O)NC3CCCCC3)CCC2C)n1 Storage condition 2-8°C Water Solubility DMSO: ≥10mg/mL |
| Use of | GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM. Properties Name (3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl]-N-cyclohexyl-6-methylpiperidine-3-carboxamide Synonym More Synonyms GSK2334470 Biological Activity Description GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM. Related Catalog Signaling Pathways >> PI3K/Akt/mTOR >> PDK-1 Research Areas >> Cancer IC50: 10 nM(PDK1)[1] In Vitro Small molecule GSK2334470 inhibits PDK1 with an IC50 of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. Addition of GSK2334470 ablates T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1). GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR, respectively, and induce higher G0-G1 ratio in LAN-1-MK than that in LAN-1 as well. PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines[2]. In Vivo The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten−/−mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1[3]. Cell Assay GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2]. References [1]. Najafov A, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J.?2011 Jan 15;433(2):357-69. [2]. Qi L, et al. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int.?2015 Sep 29;15:91. [3]. Scortegagna M, et al. 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. Chemical & Physical Properties Molecular Formula C25H34N8O Exact Mass 462.285553 PSA 132.30000 Appearance of Characters white to light brown Index of Refraction 1.667 InChIKey QLPHOXTXAKOFMU-WBVHZDCISA-N |
| Transport Info | Product name: Purity: 98.0% |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN dangerous goods number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: Non-dangerous goods IMDG Code: Non-dangerous goods International air transport dangerous goods regulations: non-dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special reminder to users No data available |
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