A rapamycin derivative
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Everolimus

Item No. 11597

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
42-O-(2-hydroxyethyl)-rapamycin
CAS Number
159351-69-6
Synonyms
  • RAD001
Molecular Formula
C53H83NO14
Formula Weight
958.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:4): 0.1 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
268, 277, 289 nm
SMILES
O=C([C@]1([H])CCCCN1C(C([C@@]2(O)[C@H](C)CC[C@](C[C@H](OC)/C(C)=C/C=C/C=C/[C@H](C3)C)([H])O2)=O)=O)O[C@](CC([C@H](C)/C=C(C)/[C@@H](O)[C@@H](OC)C([C@@H]3C)=O)=O)([H])[C@H](C)C[C@H]4C[C@@H](OC)[C@H](OCCO)CC4
InChi Code
InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-
InChi Key
HKVAMNSJSFKALM-GKUWKFKPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $54

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    10 mg

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    25 mg

    $162

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    50 mg

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    Product Description

    Everolimus is a hydroxyethyl ether rapamycin (Item No. 13346) derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.1,2 It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.2 Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.2,3 It also acts as an immunosuppressive agent in the context of organ transplantation.2,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zeng, Z., Sarbassov, D.D., Samudio, I.J., et al. Rapamycin derivatives reduce mTORC2 signaling and inhibit AKT activation in AML. Blood 109(8), 3509-3512 (2007).

    2. Lebwohl, D., Anak, Ö., Sahmoud, T., et al. Development of everolimus, a novel oral mTOR inhibitor, across a spectrum of diseases. Ann. N. Y. Acad. Sci. 1291, 14-32 (2013).

    3. Yunokawa, M., Koizumi, F., Kitamura, Y., et al. Efficacy of everolimus, a novel mTOR inhibitor, against basal-like triple-negative breast cancer cells. Cancer Sci. 103(9), 1665-1671 (2012).

    4. Gurk-Turner, C., Manitpisitkul, W., and Cooper, M. A comprehensive review of everolimus clinical reports: A new mammalian target of rapamycin inhibitor. Transplantation 94(7), 659-668 (2012).