Everolimus of MTOR Inhibitor

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Beijing
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Long-term effective
Last update:
2021-02-07 03:14
Browse the number:
194

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Product details

Research Only! We don’t sell for human use.
Everolimus, also known as RAD001 or SDZ-RAD, is an effective mTOR inhibitor derived from Rapamycin. Its immunosuppressive activity is useful in prevention of organ transplant rejection. Moreover, Everolimus is also effective in treatment of renal cell carcinoma (RCC) and other tumors by its anti-tumor activity. Everolimus binds to FKBP12 receptor to generate an everolimus-FKBP12 complex. Everolimus also has the property of inducing cell apoptosis and autophagy.

CAS No.	159351-69-6
Purity	99.10%
Target	mTOR
IC50	5-6 nM
In Vitro	The anti-proliferative concentrations of Everolimus, in the insensitive human cervical KB-31 (IC50, 1,778 nM) and the sensitive murine B16/BL6 melanoma (IC50, 0.7 nM), has caused total dephosphorylation of S6K1 and the substrate S6 and a change in the mobility of 4E-BP1. This is an indication of a reduced phosphorylation status. Although the degrees of proliferation inhibition are different, Everolimus shows dose-dependent inhibitory effect in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells. However, the growth inhibition of Everolimus in the stem cells is not as effective as in the total cells at all tested concentrations (P<0.001). IC50 values for BT474 is 2,054 nM (29 times greater than its total cells), while IC50 for primary CSCs is 3,227 nM (21 times greater than its total cells). * Above data is for reference only. Accuracy is not confirmed.
In Vivo	Everolimus has oral activity in both mice and rats. Instead of making tumor regressions, Everoliums produces an anti-tumor effect by dramatically reducing the tumor growth rates. In the rat CA20498 model, the daily dose-dependent treatment of 0.5 or 2.5 mg/kg has achieved growth inhibition with Everolimus. And similar anti-tumor effect is also produced in an intermittent treatment with a higher dose of 5 mg/kg, once or twice per week. Inhibition by Everoliums has nothing to do with any body weight loss. The effect of treatment with Everolimus (0.1-10mg/kg/d) is selective and is different from the effects of PTK/zk (100 mg/kg). * Above data is for reference only. Accuracy is not confirmed.
Formula	C₅₈H₈₈NO₁₄
SMILES	O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](OCCO)CC4)OC)C)=O)=O
M. Weight	958.2
Storage	Powder: -20°C 3 years 4°C 2 years In solvent: -80°C 6 months -20°C 1 month
Solvent & Solubility
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