2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671
PF-4708671
CAS: 1255517-76-0
Molecular Formula: C19H21F3N6
2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671 - Names and Identifiers
2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671 - Physico-chemical Properties
| Molecular Formula | C19H21F3N6 |
| Molar Mass | 390.41 |
| Solubility | DMSO: ≥20mg/mL |
| Appearance | powder |
| Color | off-white |
| Storage Condition | room temp |
| MDL | MFCD18086922 |
| Use | PF-4708671 is a p70 ribosomal S6 kinase 1(S6K1) inhibitor that can penetrate into the cell, Ki and IC50 are 20 nM and 160 nM respectively |
| In vitro study | PF-4708671 is a piperazinyl Pyrimidine analog and was the first S6K1 specific inhibitor. PF-4708671 does not significantly inhibit closely related S6K2 subtypes or a group of other AGC kinases (Akt1, Akt2, PKA, pkcα, pkc↑, PRK2, ROCK2, RSK1, RSK2 or SGK1) the activity. PF-4708671 inhibits S6K1-mediated phosphorylation of S6 protein in response IGF-1 (insulin-like growth factor 1) and has no effect on PMA-induced substrate phosphorylation, the substrates are highly related to RSK (p90 ribosomal S6 kinase) and MSK (mitogen and stress-activated protein kinase) kinases. PF-4708671 induces phosphorylation of the T-loop and hydrophobic motif of S6K1, which is dependent on mTORC1 (mTOR complex 1). PF-4708671 does not affect the activity of mTORC1. |
| In vivo study | The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment. |
2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671 - Reference
| Reference Show more | Note: part of our products can only provide part of the information, our company does not guarantee the authority of the information provided, only for the customer reference Exchange research. configuration solution concentration reference: 1mg5mg10mg1mm2.561 ml12.807 ml25.614 ml5mm0.512 ml2.561 ml5.123 ml10mm0.256 ml1.281 ml2.561 ml50mm0.051 ml0.256 ml0.512 ml storage conditions: -20 ° C PF-4708671 is a novel cell-permeatable inhibitor of S6K1 (p70 rbosomal S6 kinase 1), with a Ki of 20 nM and IC50 of 160 nM. IC50 Value: 160 nM [1] Target: S6K1 PF-4708671 is a novel cell-permeable inhibitor of S6K1, which specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM. PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1) while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 was also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 is the first S6K1-specific inhibitor to be reported and will be a useful tool for delineating S6K1-specific roles downstream of mTOR [1]. |
2-[[4-(5-Ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-1H-benzimidazole PF-4708671 - Reference Information
| biological activity | PF-4708671 is a cell permeability p70 ribosomal S6 kinase(S6K1 subtype) inhibitor. in cell-free test, Ki/IC50 is 20 nM/160 nM, acting on S6K1 is 400 times higher than acting on S6K2, and acting on S6K1 is 4 and 20 times higher than acting on MSK1 and RSK1/2, respectively, is the first reported S6K1 specific inhibitor. |
| target | TargetValue p70 s6k1 (cell-free say) 160 nm |
| Target | Value |
| p70 S6K1 (Cell-free assay) | 160 nM |
| In vitro research | PF-4708671 is a piperazinyl pyrimidine analog and the first S6K1 specific inhibitor. PF-4708671 did not significantly inhibit the activity of closely related S6K2 isoforms or a group of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKCξ, PRK2, ROCK2, RSK1, RSK2 or SGK1). PF-4708671 inhibits S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1) and has no effect on PMA-induced substrate phosphorylation. The substrate is highly related to RSK (p90 ribosomal S6 kinase) and MSK (mitogen and stress-activated protein kinase) kinase. PF-4708671 induces T-ring and hydrophobic motif phosphorylation of S6K1, which is dependent on mTORC1 (mTOR complex 1). PF-4708671 does not affect the activity of mTORC1. |
| in vivo study | the tumor growth rate in mice treated with the combination of OSI-906 + PF-4708671 is significantly than that of OSI-906 alone (P = 0.0189) or PF4708671 alone (P = 0.0165) treated mice. the average volume in the OSI-906 + PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P = 0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment. |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: PF-4708671 Visit Supplier Webpage Request for quotationCAS: 1255517-76-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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