PF-4708671 dihydrochloride | S6K1 inhibitor

CAS:
125517-76-0 (free base)
Catalog Number:
10-4856
Activity:
S6K1 inhibitor
Chemical Names:
2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzimidazole dihydrochloride
Molecular Weight:
463.33
Molecular Formula:
C19H21F3N6·2HCl
Solubility:
Soluble in DMSO (at least 35 mg/ml); Water (at least 50 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 1 month. Hygroscopic solid – protect from moisture.
Shipping Code:
RT

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5 mg$40.00
25 mg$135.00
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PF-4708671 dihydrochloride (125517-76-0 free base) is a cell permeable inhibitor of p70 ribosomal S6 kinase 1 (Ki = 20 nM; IC50 = 160 nM).1 Selective against 87 kinases including 13 other AGC family members. It enhanced cell death induced by glucose deprivation in breast cancer cells2 and inhibited cell migration in triple-negative breast cancer cells3. PF-4708671 inhibited cell proliferation and invasiveness in multiple non-small cell lung cancer cell lines and inhibited tumorigenesis in mice.4 It induced AMPK phosphorylation and activation independently of p70SK1 via specific inhibition of mitochondrial respiratory chain complex I.5 PF-4708671 displayed protective effects in a mouse model of cerebral ischemia-reperfusion injury.6

References/Citations:

  1. Pearce et al. (2010) Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1); Biochem. J. 431 245
  2. Choi et al. (2013) Inhibition of S6K1 enhances glucose deprivation-induced cell death via downregulation of anti-apoptotic proteins in MCF-7 breast cancer cells; Biochem. Biophys. Res. Commun. 432 123
  3. Khotskaya et al. (2014) S6K1 promotes invasiveness of breast cancer cells in a model of metastasis of triple-negative breast cancer; Am. J. Transl. Res. 6 361
  4. Qiu et al. (2016) The p70S6K Specific Inhibitor PF-4708671 Impedes Non-Small Cell Lung Cancer Growth; PLoS One, 11 e0147185
  5. Vainer et al. (2014) PF-4708671 activates AMPK independently of p70S7K1 inhibition; PLoS One, 9 e107364
  6. Chi et al. (2019) Inhibition of p70 ribosomal S6 kinase 1 (S6K1) by PF-7408671 decreased infarct size in early cerebral ischemia-reperfusion with decreased BBB permeability; PLoS One, 9 e107364
CAS:
125517-76-0 (free base)
Catalog Number:
10-4856
Activity:
S6K1 inhibitor
Chemical Names:
2-[[4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl]methyl]-5-(trifluoromethyl)-1H-benzimidazole dihydrochloride
Molecular Weight:
463.33
Molecular Formula:
C19H21F3N6·2HCl
Solubility:
Soluble in DMSO (at least 35 mg/ml); Water (at least 50 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 1 month. Hygroscopic solid – protect from moisture.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Download Product Data Sheet

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

PF-4708671 dihydrochloride (125517-76-0 free base) is a cell permeable inhibitor of p70 ribosomal S6 kinase 1 (Ki = 20 nM; IC50 = 160 nM).1 Selective against 87 kinases including 13 other AGC family members. It enhanced cell death induced by glucose deprivation in breast cancer cells2 and inhibited cell migration in triple-negative breast cancer cells3. PF-4708671 inhibited cell proliferation and invasiveness in multiple non-small cell lung cancer cell lines and inhibited tumorigenesis in mice.4 It induced AMPK phosphorylation and activation independently of p70SK1 via specific inhibition of mitochondrial respiratory chain complex I.5 PF-4708671 displayed protective effects in a mouse model of cerebral ischemia-reperfusion injury.6

References/Citations:

  1. Pearce et al. (2010) Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1); Biochem. J. 431 245
  2. Choi et al. (2013) Inhibition of S6K1 enhances glucose deprivation-induced cell death via downregulation of anti-apoptotic proteins in MCF-7 breast cancer cells; Biochem. Biophys. Res. Commun. 432 123
  3. Khotskaya et al. (2014) S6K1 promotes invasiveness of breast cancer cells in a model of metastasis of triple-negative breast cancer; Am. J. Transl. Res. 6 361
  4. Qiu et al. (2016) The p70S6K Specific Inhibitor PF-4708671 Impedes Non-Small Cell Lung Cancer Growth; PLoS One, 11 e0147185
  5. Vainer et al. (2014) PF-4708671 activates AMPK independently of p70S7K1 inhibition; PLoS One, 9 e107364
  6. Chi et al. (2019) Inhibition of p70 ribosomal S6 kinase 1 (S6K1) by PF-7408671 decreased infarct size in early cerebral ischemia-reperfusion with decreased BBB permeability; PLoS One, 9 e107364

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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21

Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21

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