Specifications
- Purity
- ≥99% (HPLC)
- Identity
- IR
- Appearance
- White to off-white powder
Properties
- Melting Point
- 107-113 °C
- Solvents
- ethanol, methanol, DMF, DMSO
Available from stock
Everolimus
- SKU
- E0074
Category: API's & Intermediates
- Synonyms
- 42-O-(2-Hydroxyethyl)rapamycin , CERTICAN® , Afinitor®
- 159351-69-6
- CAS-Number
- C53H83NO14
- Molecular Formula
- 958.22
- Molecular Weight
- Handling Advice
- Protect from light and moisture.
- Use / Stability
- Stable for at least 2 years after receipt when stored at -20°C.
- Long Term Storage
- -20°C
- Short Term Storage
- +4°C
- Shipping
- AMBIENT
- Transportation
- Not dangerous goods
- Signal word
- Danger
- GHS Symbol
- GHS08
- Precautionary statements
- P273-P314
- Hazard statements
- H372-H412
- Description
- Everolimus is a macrolide derived from rapamycin (sc-3504) with immunosuppressant properties shown to inhibit cell proliferation induced by growth factors. Macrolides belong to a group of antibiotics that bind to the 50S ribosomal subunit and inhibit protein synthesis. Studies indicate that everolimus is a mTOR (FRAP) inhibitor that displays high affinity toward the intracellular receptor FKBP12. Additionally, the Everolimus-FKBP12 complex decreases the activity of the S6K1 and 4EBP by binding to FRAP.
- InChi
- InChI=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-
- References
- (1) H.J. Schuurman, et al., Transplantation 64, 32 (1997) , (2) W. Schuler, et al., Transplantation 64, 36 (1997) , (3) P. Neuhaus, et al., Liver Transpl. 7, 473 (2001) (Review) , (4) B. Nashan, Expert Opin. Investig. Drugs. 11, 1845 (2002) (Review) , (5) I. Beuvink, et al., Cell 120, 747 (2005) , (6) J.K. Patel & J.A. Kobashigawa, Expert Opin. Pharmacother. 7, 1347 (2006) (Review) , (7) P. Smolewski, Anticancer Drugs 17, 487 (2006) (Review) , (8) K. Zitzmann, et al., Neuroendocrinology 85, 54 (2007) , (9) Z. Zeng, et al., Blood 109, 3509 (2007) , (10) R. Bianco, et al., Br. J. Cancer 98, 923 (2008) , (11) A.I. Sanchez-Fructuoso, Expert Opin. Drug Metab. Toxicol. 4, 807 (2008) (Review) , (12) H.A. Lane, et al., Clin. Cancer Res. 15, 1612 (2009) , (13) D. Lebwohl, et al., Ann. N. Y. Acad. Sci. 1291, 14 (2013) (Review) , (14) U. Saran, et al., Clin. Sci. 129, 895 (2015) (Review) , (15) Morviducci, et al., Diabetes Res. Clin. Pract. (Epub ahead of print) (2018) (Review)
- InChi Key
- HKVAMNSJSFKALM-GKUWKFKPSA-N
- Smiles
- CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OCCO)C)C)O)OC)C)C)C)OC
Everolimus is a macrolide derived from rapamycin (sc-3504) with immunosuppressant properties shown to inhibit cell proliferation induced by growth factors. Macrolides belong to a group of antibiotics that bind to the 50S ribosomal subunit and inhibit protein synthesis. Studies indicate that everolimus is a mTOR (FRAP) inhibitor that displays high affinity toward the intracellular receptor FKBP12. Additionally, the Everolimus-FKBP12 complex decreases the activity of the S6K1 and 4EBP by binding to FRAP.
Additional information
| Synonyms | 42-O-(2-Hydroxyethyl)rapamycin, CERTICAN®, Afinitor® |
|---|---|
| Purity | ≥99% (HPLC) |
| Appearance | White to off-white powder |
| CAS-Number | 159351-69-6 |
| Molecular Formula | C53H83NO14 |
| Molecular Weight | 958.22 |
| Identity | IR |
| Solvents | ethanol, methanol, DMF, DMSO |
| Melting Point | 107-113 °C |
| Smiles | CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OCCO)C)C)O)OC)C)C)C)OC |
| InChi Key | HKVAMNSJSFKALM-GKUWKFKPSA-N |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Protect from light and moisture. |
| Use / Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Hazard statements | H372-H412 |
| Precautionary statements | P273-P314 |
| GHS Symbol | GHS08 |
| Signal word | Danger |
| Transportation | Not dangerous goods |
| References | (1) H.J. Schuurman, et al., Transplantation 64, 32 (1997), (2) W. Schuler, et al., Transplantation 64, 36 (1997), (3) P. Neuhaus, et al., Liver Transpl. 7, 473 (2001) (Review), (4) B. Nashan, Expert Opin. Investig. Drugs. 11, 1845 (2002) (Review), (5) I. Beuvink, et al., Cell 120, 747 (2005), (6) J.K. Patel & J.A. Kobashigawa, Expert Opin. Pharmacother. 7, 1347 (2006) (Review), (7) P. Smolewski, Anticancer Drugs 17, 487 (2006) (Review), (8) K. Zitzmann, et al., Neuroendocrinology 85, 54 (2007), (9) Z. Zeng, et al., Blood 109, 3509 (2007), (10) R. Bianco, et al., Br. J. Cancer 98, 923 (2008), (11) A.I. Sanchez-Fructuoso, Expert Opin. Drug Metab. Toxicol. 4, 807 (2008) (Review), (12) H.A. Lane, et al., Clin. Cancer Res. 15, 1612 (2009), (13) D. Lebwohl, et al., Ann. N. Y. Acad. Sci. 1291, 14 (2013) (Review), (14) U. Saran, et al., Clin. Sci. 129, 895 (2015) (Review), (15) Morviducci, et al., Diabetes Res. Clin. Pract. (Epub ahead of print) (2018) (Review) |
| InChi | InChI=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- |
| Quantity | 100 mg, 250 mg, Bulk |
