- WYE-354
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- $43.00
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2026-04-21
- CAS:1062169-56-5
- Purity: 98.31%
- Supply Ability: 10g
- WYE-354
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- $2.00
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2019-07-06
- CAS:1062169-56-5
- Min. Order: 1kg
- Purity: 99%
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| | WYE-354 Basic information |
| | WYE-354 Chemical Properties |
| density | 1.46 | | storage temp. | Sealed in dry,Store in freezer, under -20°C | | solubility | ≥49.6 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | 13.42±0.70(Predicted) | | color | White to off-white | | InChIKey | IMXHGCRIEAKIBU-UHFFFAOYSA-N | | SMILES | N1(C(OC)=O)CCC(N2C3C(C=N2)=C(N2CCOCC2)N=C(C2=CC=C(NC(OC)=O)C=C2)N=3)CC1 |
| | WYE-354 Usage And Synthesis |
| Description | WYE-354 is a potent cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTOR complex 1 (mTORC1) and mTORC2. It is a much weaker inhibitor of phosphatidylinositol 3-kinase α (IC50 = 1,026 nM) and other kinases. WYE-354 induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines, inhibits mTORC1 and mTORC2 in tumor-bearing mice, and reduces tumor growth in nude mice with PTEN-null tumors. | | Uses | A pyrazolopyrimidines derivative that is a potent and ATP-competitive mTOR inhibitor with much reduced activity against PI 3-Kα or PI 3-Kγ. WYE-354 is equally potent against mTORC1 and mTORC2 activities in HEK293 immune complex kinase assays using S6K and Akt as the respective substrate (IC50 <200 nM; [ATP] = 100 μM) and effectively blocks cellular phosphorylation of S6K on T389 and Akt on S473 both in cultures and in a murine xenograft model, resulting in a significant suppression of PC3MM2-derived tumor growth (by 86% on day 7; 50 mg/kg, i.p twice per day) in vivo. | | Definition | ChEBI: 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester is a carbamate ester. | | in vivo | The effect of Rapamycin and WYE-354 on tumor growth is evaluated in xenograft GBC tumor models. 2×106 or 5×106 cells of G-415 or TGBC2TKB, respectively, are xenotransplanted into NOD-SCID mice subcutaneously. When tumors reach an average volume of 100 mm3, the mice are treated either with Rapamycin or WYE354. Rapamycin is administered i.p. at a concentration of 10 mg/kg, daily for 5 days per week for 3 weeks, while WYE-354 is administrated at a daily i.p. dose of 50 mg/kg for 5 days. Mice are sacrificed 30 days after the initiation of the treatments and an autopsy is performed that include removal of the entire tumor area. Mice treated with WYE-354 exhibit 68.6% and 52.4% reduction in average tumor size (P<0.01; P<0.01), as well as 82.9% and 45.5% (P<0.01; ns) reduction in tumor weight, respectively[2]. | | target | mTOR | | IC 50 | mTOR: 5 nM (IC50); mTORC1; mTORC2; PI3K alpha: 1.89 μM (IC50); PI3K gamma: 7.37 μM (IC50); Autophagy | | references | [1] qingsong liu, carson thoreen, jinhua wang, david sabatini, nathanael s. gray. mtor mediated anti-cancer drug discovery. drug discovery today. 2009. 6(2): 47-55.
[2] shi-yong sun. mtor kinase inhibitors as potential cancer therapeutic drugs. cancer letters. 28 october 2013. 340(1): 1-8. |
| | WYE-354 Preparation Products And Raw materials |
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