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Everolimus

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.

Please kindly note that our products and services can only be used to support research purposes (Not for clinical use).

CAT No: Z10-101-155

CAS No: 159351-69-6

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cGMP Peptide

Registration of APIs CMC information required for an IND

IND and NDA support Drug master files (DMF) filing

Synonyms/AliasAfinitor; Certican; Zortress; RAD001; SDZ-RAD
M.F/FormulaC53H83NO14
M.W/Mr.958.24
Labeling TargetSerine/threonine-protein kinase mTOR
ApplicationEverolimus 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.
AppearanceWhite to off-white solid powder
Purity>98% (or refer to the Certificate of Analysis)
ActivityInhibitor
Biological ActivityEverolimus, also known as RAD001, is a derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties.
Areas of InterestKinase Inhibitor
FunctionsTfiiic-class transcription factor binding
TargetmTOR
Long-term Storage ConditionsSoluble in DMSO, not in water
Shipping ConditionShipped 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 ConditionsDry, dark and at 0 - 4 °C
Solubility-20 °C
OrganismHuman
InChIInChI=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 KeyHKVAMNSJSFKALM-GKUWKFKPSA-N
Isomeric SMILESC[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
BoilingPoint998.7±75.0 °C at 760 mmHg
ShelfLife>2 years if stored properly
Melting PointN/A
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