98% Min MTOR Inhibitors PP121 Cas 1092788-83-4
98% Min MTOR Inhibitors PP121 Cas 1092788-83-4
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Chemical Information
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Product name:PP121 |
Purity:98% min |
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CAS NO:1092788-83-4 |
Solubility:DMSO20 mg/mL (62.63 mM) |
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Molecular Formula:C17H17N7 |
Package:Package according to customer requirements |
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Molecular Weight:319.364 |
Storage:Store at -20℃ |
Quality control
Remarks
PP121 blocks the PI3K pathway by direct inhibition of PI3K/mTOR in two glioblastoma cell lines, U87 and LN229. PP121 potently inhibits the proliferation of a diverse panel of tumor cell lines containing mutations in the PI3-K pathway components PIK3CA, PTEN, or RAS. PP121 induces a G0G1 arrest in most tumor cells.
PP121 directly inhibits Src in cells and reverses its biochemical and morphological effects. PP121 potently inhibits the Ret kinase domain in vitro (IC50<1 nM). PP121 potently blocks VEGF stimulated activation of the PI3-K and MAPK pathways. PP121 inhibits VEGFR2 autophosphorylation at low nanomolar concentrations, confirming that this molecule directly targets VEGFR2 in cells.
PP121 inhibits Bcr-Abl induced tyrosine phosphorylation in K562 cells as well as BaF3 cells that express Bcr-Abl.
Related Prodcuts:
Tacrolimus; AZD8055; AZD8055 fumarate; OSI-027; Vistusertib; Zotarolimus; XL388; INK 128; Desmethyl-VS-5584; AZD-8055
References
[1]. Apsel B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 2008, 4(11), 691-699.
[2]. Peng Y, et al. The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121. Biochem Biophys Res Commun. 2015 Sep 11; 465(1):137-44.
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