Rapamycin --- mTOR inhibitor

Rapamycin is a potent and selective mTOR inhibitor. Rapamycin, in complex with the cytosolic protein FK-binding protein 12 (FKBP12), inhibits mTOR Complex 1 (mTORC1) by binding to the FRB domain of mTor. Given the central roles mTor plays, Rapamycin showed diverse activities, including anti-proliferative effects in cancer cells, immunosuppressive effect, lifespan extension in mice, improved cognition in the mouse model of autism and Alzheimer, and inducing autophagy.

Product information

CAS Number: 53123-88-9

Molecular Weight: 914.17

Formula: C51H79NO13

Chemical Name: (3S, 6R, 7E, 9R, 10R, 12R, 14S, 15E, 17E, 19E, 21S, 23S, 26R, 27R, 34aS)- 9, 10, 12, 13, 14, 21, 22, 23, 24, 25, 26, 27, 32, 33, 34, 34a-hexadecahydro-9, 27-dihydroxy-3- [(1R)-2-[(1S, 3R, 4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10, 21-dimethoxy-6, 8, 12, 14, 20, 26- hexamethyl-23, 27-epoxy-3H-pyrido[2, 1-c][1, 4]-oxaazacyclohentriacontine-1, 5, 11, 28, 29 (4H, 6H, 31H)- pentone

Smiles: CC1=C[C@@H](C)C(=O)C[C@H](OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@H](C[C@H](OC)C(C)=CC=CC=C[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@@H]1O)CC[C@H]2C)[C@H](C)C[C@H]1C[C@@H](OC)[C@H](O)CC1 |c:1,t:32,34,36|

InChiKey: QFJCIRLUMZQUOT-BLBZBZKNSA-N

InChi: InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11-,16-12-,31-17-,35-25-/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Rapamycin is usually used at 1 µM final concentration in vitro and in cellular assays.

In Vivo:

Rapamycin could be orally administrated to mice at 5-20 mg/kg once per day.

References:

1. Vézina C, et al. Rapamycin (AY-22,989), a new antifungal antibiotic. (1975) J. Antibiot. 28 (10): 721.
2. Heitman J, et al. Targets for cell cycle arrest by the immunosuppressant rapamycin in yeast. (1991) Science. 253: 905-909.
3. Price DJ, et al. Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase. (1992) Science. 257: 973-977.
4. Wells AD, et al. Requirement for T-cell apoptosis in the induction of peripheral transplantation tolerance. (1999) Nat. Med.5:1303-1307.

Products are for research use only. Not for human use.

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