Everolimus is a Kinase Inhibitor and mTOR Inhibitor Immunosuppressant. The mechanism of action of everolimus is as a Protein Kinase Inhibitor and Cytochrome P450 3A4 Inhibitor and P-Glycoprotein Inhibitor and Cytochrome P450 2D6 Inhibitor and mTOR Inhibitor. The physiologic effect of everolimus is by means of Decreased Immunologic Activity.
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IND and NDA support Drug master files (DMF) filing
Synonyms/Alias | Afinitor; Certican; Zortress; RAD001; SDZ-RAD |
M.F/Formula | C53H83NO14 |
M.W/Mr. | 958.24 |
Labeling Target | Serine/threonine-protein kinase mTOR |
Application | Everolimus is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein. |
Appearance | White to off-white solid powder |
Purity | >98% (or refer to the Certificate of Analysis) |
Activity | Inhibitor |
Biological Activity | Everolimus, also known as RAD001, is a derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. |
Areas of Interest | Kinase Inhibitor |
Functions | Tfiiic-class transcription factor binding |
Target | mTOR |
Long-term Storage Conditions | Soluble in DMSO, not in water |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
Short-term Storage Conditions | Dry, dark and at 0 - 4 °C |
Solubility | -20 °C |
Organism | Human |
InChI | 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/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1 |
InChI Key | HKVAMNSJSFKALM-GKUWKFKPSA-N |
Isomeric SMILES | C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OCCO)C)/C)O)OC)C)C)/C)OC |
BoilingPoint | 998.7±75.0 °C at 760 mmHg |
ShelfLife | >2 years if stored properly |
Melting Point | N/A |
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