Manufacturer with High Purity and Stable Quality
Chemical Name: Rapamycin
CAS: 53123-88-9
Antifungal and Antineoplastic Agent
API High Quality, Commercial Production
| Chemical Name |
Rapamycin |
| Synonyms |
Sirolimus; AY-22989 |
| CAS Number |
53123-88-9 |
| CAT Number |
RF-API59 |
| Stock Status |
In Stock, Production Scale Up to Hundreds of Kilograms |
| Molecular Formula |
C51H79NO13 |
| Molecular Weight |
914.19 |
| Brand |
Ruifu Chemical |
| Item |
Specifications |
| Appearance |
White Crystalline Powder, Odourless |
| Solubility |
Freely soluble in methanol, chloroform, soluble in ethanol, ethyl acetate, Practically Insoluble in petroleum ether, water |
| Assay |
≥98.0% (HPLC) |
| Optical Rotation |
-147.0° -157.0° (MeOH) |
| Loss on Drying |
≤1.0% |
| Melting Point |
183.0~185.0℃ |
| Heavy Metals |
≤20ppm |
| Test Standard |
Enterprise Standard; National Medical Products Administration (NMPA) |
| Usage |
Active Pharmaceutical Ingredient (API) |
Package: Bottle, Aluminum foil bag, Cardboard drum, 25kg/Drum, or according to customer's requirement.
Storage Condition: Store in sealed containers at cool and dry place; Protect from light, moisture and pest infestation.
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant. Rapamycin (Rapa, or Sirolimus) is a new form of macrolide immunosuppressive agent. It is a white solid crystal. Its melting point is 183-185℃ and it is lipophilic. It is soluble in methanol, ethanol, acetone, chloroform, and other organic solvents, very slightly soluble in water, and almost insoluble in ether. It was first discovered in 1975 on the Chilean Easter Island as a secondary metabolite secreted by soil Streptomyces, and its chemical structure is that of a three-polyene macrolide compound. Rapamycin is a new form of immunosuppressive agent with good curative effects, low toxicity, and no nephrotoxicity. It can be used to maintain the immunity of transplant organs (especially in kidney transplants) to alleviate immunological rejections after organ transplant surgeries. The latest research has shown that Rapamycin can also be used to treat Alzheimer’s. When used on afflicted lab rats, it had a memory-restoring effect. Rapamycin oral tablets can be taken with grapefruit juice to treat melanoma (a type of benign tumor common among Western populations), dramatically increase other chemotherapy drugs’ anticancer effects, and extend patient survival. Rapamycin is a mammalian target of rapamycin (mTOR) targeting inhibitor, which can treat tumors that are related to this pathway including kidney cancer, lymphoma, lung cancer, liver cancer, breast cancer, neuroendocrine carcinoma, gastric cancer, etc. Its curative effects are especially strong for the rare diseases LAM (lymphangiomyomatosis) and TSC (tuberous sclerosis).
Rapamycin is a member of the macrolide immunosuppressant family and a FRAP inhibitor. Rapamycin exhibits binding and inhibitory actions to the FK506 binding protein (FKBP5) proline rotamase via simultaneous binding by FKBP12 and FRAP. FRAP (RAFT1) proteins exhibit homology to PI 4- and PI 3-kinases, which have PI 4-kinase and autophosphorylating activities. The rapamycin/FKBP complex does not inhibit the FRAP PI 4-kinase activity, but does inhibit FRAP autophosphorylation. Rapamycin is unique in its ability to inhibit lymphokine induced cell proliferation at the G1 and S phase as well as an irreversible cellular arrest at the G1 phase in S. cerevisiae cells. Rapamycin also exhibits selective signal blocking leading to the activation of p70/85 S6 kinase, which is potentially due to the inhibition of FRAP autophosphorylation or protein kinase activity. Rapamycin also exhibits Angiogenesis inhibition, possibly through the inhibition of the Akt pathway. Rapamycin is an inhibitor of mTOR.