Rapamycin Inhibitor CAS No. 53123-88-9

Cat. No.	Name	Size	Price
KI0298	Rapamycin	5 mg	$112
	Rapamycin	25 mg	$320
	Rapamycin	100 mg	$840

Chemical Characteristic

Product Name	Rapamycin
Synonyms	Sirolimus
CAS No.	53123-88-9
Molecular Weight	914.18
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-ep
Smiles	O1C(=O)[C@H]2N(C(=O)C(=O)[C@]3([C@@H](CC[C@@H](C[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)CC1[C@@H](CC1C[C@H]([C@@H](CC1)O)OC)C)C)/C)O)OC)C)C)/C)OC)O3)C)O)CCCC2
Chemical Structure

Biological activities

Rapamycin forms a complex with FK506-binding protein 12 that binds and inhibits mammalian target of TOR kinase activity, leading to dephosphorylation of downstream targets of mTOR, S6K1, and 4E-BP1. Rapamycin is an antibiotic and fungicide isolated from Streptomyces hygroscopicus.^[1] S6K1 and 4E-BP1 regulate ribosomal component biogenesis and cap-dependent mRNA translation, and their dephosphorylation inhibits translation of mRNAs involved in cell cycle, proliferation, and induction of growth arrest at G1 phase. Rapamycin potently inhibits platelet-derived growth factor (PDGF) with an IC50 of 5 nM and basic fibroblast growth factor (bFGF)-induced VSMC DNA synthesis with an IC50 of 0.8 nM. At 46 hours after growth factor addition, 1 nM rapamycin still effectively suppresses bFGF-or PDGF-induced DNA synthesis by 76% and 54%, respectively.^[2] When treating MDA-MB-468 cells (a PTEN-null human breast cancer cell line) in vitro with rapamycin at concentrations ranging from 0.1 to 1000 nM for 5 days, the IC50 of rapamycin is less than 1 nM. Rapamycin (100 nM ) treatment significantly inhibits colony-forming ability in MDA-MB-468 cells.^[3] Nanomolar concentrations of rapamycin inhibit 70% proliferation of primary murine bone marrow cells incubated for 2 days with either mIL-3, mGM-CSF, mKL, or with a combination of WEHI and L929 cell conditioned media as a source of cytokines (half-maximum inhibition, about 0.3 nM). Besides, rapamycin (0-10 µM) also inhibits the multiplication of colony-forming cells in suspension cultures containing IL-3 plus interleukin-l (IL-l) or interleukin-l1 (IL-11) plus KL. ^[4] In MDA-MB-468 cells xenografts models, a statistically significantly lower mean tumor volume on day 22 after injection in the mice given rapamycin (140 mm3) than in the control mice (355 mm3) is observed.^[3] Besides, in HepG2 cell xenograft models , mice treated with rapamycin/bevacizumab (oral administration rapamycin at 1 mg/kg and intraperitoneal injection bevacizumab at 5 mg/kg), rapamycin (oral administration at 1 mg/kg), and bevacizumab (intraperitoneal injection at 5 mg/kg) all show a marked decrease in the tandardized uptake values max (SUV _{max) readings with the greatest drop being observed in the rapamycin/bevacizumab group (1.33, 1.81, 2.05 vs. vehicle control 2.11).^[5]}

References

[1] Hidalgo M, et al. The rapamycin-sensitive signal transduction pathway as a target for cancer therapy. Oncogene. 2000, 19(56): 6680-6686. [2] Cao W, et al. Effects of rapamycin on growth factor-stimulated vascular smooth muscle cell DNA synthesis. Inhibition of basic fibroblast growth factor and platelet-derived growth factor action and antagonism of rapamycin by FK506. Transplantation. 1995, 59(3): 390-395. [3] Akcakanat A, et al. The rapamycin-regulated gene expression signature determines prognosis for breast cancer. Mol Cancer. 2009, 8: 75. [4] Quesniaux VF, et al. The immunosuppressant rapamycin blocks in vitro responses to hematopoietic cytokines and inhibits recovering but not steady-state hematopoiesis in vivo. Blood. 1994, 84(5): 1543-1552. [5] Ong LC, et al. Effective inhibition of xenografts of hepatocellular carcinoma (HepG2) by rapamycin and bevacizumab in an intrahepatic model. Mol Imaging Biol. 2009, 11(5): 334-342.

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