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

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥99% (HPLC)
Appearance: White to off-white powder
Identity: IR

Properties

Solvents: ethanol, methanol, DMF, DMSO
Melting Point: 107-113 °C

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

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.
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
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-

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.

SKU: E0074 Category: API's & Intermediates

Additional information

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