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ALX-380-004 Revised 21-Feb-08
Rapamycin
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SYNONYMS Sirolimus
AY-22,989
RAPA
Rapamune
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Immunomodulators
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-004-C100   100 µg 35.00 USD Add To Cart
ALX-380-004-5100   5x100 µg 90.00 USD Add To Cart
ALX-380-004-M001   1 mg 120.00 USD Add To Cart
ALX-380-004-M005   5 mg 420.00 USD Add To Cart
ALX-380-004-M025   25 mg 950.00 USD Add To Cart
Product Specification
FORMULA: C51H79NO13
MW: 914.2
CAS NUMBER: 53123-88-9
MERCK INDEX: 14: 8114
RTECS: VE6250000
SOURCE/HOST: Isolated from Streptomyces hygroscopicus.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in chloroform, DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Macrocyclic-triene antibiotic possessing potent immunosuppressant activity. It forms a complex with FKBP12 that binds to an effector, thus inhibiting IL-2 and other growth promoting lymphokines. The effectors were recently identified as FRAP (FKBP12 rapamycin-associated protein) and RAFT1 (rapamycin and KFBP12 target). Rapamycin induces inhibition of p70s6k, p33cdk2 and p34cdc2. Enhances apoptosis.
Product Specific Literature References
Rapamycin (AY-22,989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle: C. Vezina, et al.; J. Antibiot. (Tokyo) 28, 721 (1975) Abstract
Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization: S.N. Sehgal, et al.; J. Antibiot. (Tokyo) 28, 727 (1975) Abstract
Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase: D.J. Price, et al.; Science 257, 973 (1992) Abstract
Rapamycin: in vitro profile of a new immunosuppressive macrolide: S.N. Sehgal & C.C. Bansback; Ann. N. Y. Acad. Sci. 685, 58 (1993) Abstract
Rapamycin inhibition of interleukin-2-dependent p33cdk2 and p34cdc2 kinase activation in T lymphocytes: W.G. Morice, et al.; J. Biol. Chem. 268, 22737 (1993) Abstract; Full Text
A mammalian protein targeted by G1-arresting rapamycin-receptor complex: E.J. Brown, et al.; Nature 369, 756 (1994) Abstract
RAFT1: a mammalian protein that binds to FKBP12 in a rapamycin- dependent fashion and is homologous to yeast TORs: D.M. Sabatini, et al.; Cell 78, 35 (1994) Abstract
Rapamycin, a potent immunosuppressive drug, causes programmed cell death in B lymphoma cells: S. Muthukkumar, et al.; Transplantation 60, 264 (1995) Abstract
Rapamycin enhances apoptosis and increases sensitivity to cisplatin in vitro: Y. Shi, et al.; Cancer Res. 55, 1982 (1995) Abstract
Rapamycin potentiates dexamethasone-induced apoptosis and inhibits JNK activity in lymphoblastoid cells: T. Ishizuka, et al.; BBRC 230, 386 (1997) Abstract
Rapamycin and p53 act on different pathways to induce G1 arrest in mammalian cells: S.M. Metcalfe, et al.; Oncogene 15, 1635 (1997) Abstract
Rapamycin inhibition of the G1 to S transition is mediated by effects on cyclin D1 mRNA and protein stability: S. Hashemolhosseini, et al.; J. Biol. Chem. 273, 14424 (1998) Abstract; Full Text
Rapamycin causes poorly reversible inhibition of mTOR and induces p53- independent apoptosis in human rhabdomyosarcoma cells: H. Hosoi, et al.; Cancer Res. 59, 886 (1999) Abstract
Rapamycin: an anti-cancer immunosuppressant?: B.K. Law; Crit. Rev. Oncol. Hematol. 56, 47 (2005), Review Abstract
mTOR inhibitors (rapamycin and its derivatives) and nitrogen containing bisphosphonates: bi-functional compounds for the treatment of bone tumours: B. Ory, et al.; Curr. Med. Chem. 14, 1381 (2007), Review Abstract
 
 

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