Tenifatecan | SN-2310 | CAS#850728-17-5

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MedKoo product information:

Tenifatecan

Description of Tenifatecan: Tenifatecan, also known as SN2310, is an injectable emulsion composed of 7-ethyl-10-hydroxycamptothecin (SN-38) conjugate with vitamin E through a succinate linker. SN-38 is the active metabolite of irinotecan. SN-38 binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication, and apoptosis. SN-38 has been reported to exhibit up to 1,000-fold more cytotoxic activity against various cancer cells in vitro than irinotecan. SN2310 Injectable Emulsion is being developed with the objective of demonstrating improved anti-tumor activity as a result of increased exposure to SN-38 based on a longer half-life.

Current developer: OncoGenex Pharmaceuticals Inc.

MedKoo Code#: 202630

Name: Tenifatecan

CAS#: 850728-17-5

Synonym: SN 2300; BEL2310; Tocopherol succinate camptothecin; d-.alpha.-Tocopherol succinate camptothecin.

IUPAC/Chemical name:

(S)-4-ethyl-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-4-yl ((R)-2,5,7,8-tetramethyl-2-((4R,8R)-4,8,12-trimethyltridecyl)chroman-6-yl) succinate

Chemical structure:

Theoretical analysis :

Chemical Formula: C53H68N2O8

Exact Mass: 860.49757

Molecular Weight: 861.1

Elemental Analysis: C, 73.92; H, 7.96; N, 3.25; O, 14.86

Availability and price:

This agent is not in stock, and is available through custom synthesis.

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Quality control data:

Product will be shipped with supporting analytical data.

Information about this agent

SN2310 is a novel camptothecin for the treatment of cancer. Camptothecins are potent anticancer agents that belong to the family of drugs called topoisomerase I inhibitors that bind reversibly to the TOPO-I-DNA complex causing breaks in the DNA strands during replication resulting in cell death. SN2310 Injectable Emulsion is an oil-and-water emulsion that incorporates a new derivative of SN-38, SN2310. The conjugation of SN-38 to Vitamin E succinate enables increased solubility in a vitamin E-based, oil-in-water emulsion that can be administered without dilution. The difference in the structure is shown in the right sidebar. SN2310 Injectable Emulsion is being developed with the objective of demonstrating improved anti-tumor activity as a result of increased exposure to SN-38 based on a longer half-life. In addition, the product is more convenient, with a shorter duration of administration and no requirement for reconstitution. (from: http://www.oncogenex.ca/products/SN2310.html).

References

1. Zhang, Yuehua; Gold, Lynn C. Preparation of tocopherol-modified pharmaceuticals. U.S. Pat. Appl. Publ. (2005), 42 pp. CODEN: USXXCO US 2005096340 A1 20050505 CAN 142:435789 AN 2005:394830 CAPLUS

2. Zhang, Yuehua; Gold, Lynn C. Tocopherol modified therapeutic drug compounds. U.S. Pat. Appl. Publ. (2008), 67pp., Cont.-in-part of U. S. Ser. No. 450,795. CODEN: USXXCO US 2008045559 A1 20080221 CAN 148:262770 AN 2008:224479 CAPLUS

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