TPI-287 | ARC-100

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MedKoo product information:

TPI-287

MedKoo Code#: 202964
Name: TPI-287
CAS#: 849213-15-6 Synonym: Code name: TPI-287.ARC-100. CA Index Name: Hexanoic acid, 3-[[(1,1-dimethylethoxy)carbonyl]amino]-2-hydroxy-5-methyl-, (1S,2S,4S,7S,7aR,10aS,11aR,13aS,13bR,13cS)-7,13a-bis(acetyloxy)-1-(benzoyloxy)-9-ethenyl-1,3,4,7,7a,10a,11,11a,13,13a,13b,13c-dodecahydro-2-hydroxy-5,13c,14,14-tetramethyl-2,6-methano-2H-cyclodec[de]oxeto[3,2-g][1,3]benzodioxin-4-yl ester, (2R,3S)-. Other Names: TPI 287 　 IUPAC/Chemical name: (1S,2S,4S,7S,7aR,7a1S,10aS,11aR,13aS,13bR)-1-(benzoyloxy)-4-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-5-methylhexanoyl)oxy)-2-hydroxy-5,7a1,14,14-tetramethyl-9-vinyl-2,3,4,7,7a,7a1,10a,11,11a,13,13a,13b-dodecahydro-1H-8,10,12-trioxa-2,6-methanocyclobuta[b]cyclodeca[de]naphthalene-7,13a-diyl diacetate
Chemical structure	Theoretical analysis
	Chemical Formula: C46H63NO15 Exact Mass: 869.41977 Molecular Weight: 869.99 m/z: 869.41977 (100.0%), 870.42313 (49.8%), 871.42648 (12.1%), 871.42402 (3.1%), 872.42983 (1.9%), 872.42737 (1.5%) Elemental Analysis: C, 63.51; H, 7.30; N, 1.61; O, 27.59
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Information about this agent

TPI 287 is a synthetic, third generation taxane with potential antineoplastic activity. TPI 287 binds to tubulin and stabilizes microtubules, resulting in inhibition of microtubule assembly/disassembly dynamics, cell cycle arrest at the G2/M phase, and apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

TPI 287, a proprietary next-generation taxane, is Tapestry's lead clinical compound. This compound was designed to overcome multiple drug resistance in solid tumors that are innately resistant to taxane therapy or have become resistant to taxanes following exposure to chemotherapy drugs. In preclinical testing, TPI 287 demonstrated the ability to inhibit tumor cell growth in a number of in vitro cell lines and has shown inhibition of human tumor growth in certain animal xenograft models when tested against standard comparative agents. The in vitro activity was seen across multiple cell lines including cell lines known to be sensitive to taxanes as well as cell lines known to be resistant to taxanes. Taxane sensitive cell lines in which TPI 287 has shown activity include cell lines derived from breast cancer, uterine cancer and non-small cell lung cancer. Taxane resistant cell lines in which TPI 287 has shown activity include cell lines derived from breast cancer, colon cancer and prostate cancer. See http://www.tapestrypharma.com.

Current developer: Tapestry Pharmaceuticals, Inc./Archer Biosciences Incorporated

References

1. Mann, David Marshall. Gene expression profiling in the pulmonary artery in the selection of therapies for vascular-related diseases. PCT Int. Appl. (2009), 115pp. CODEN: PIXXD2 WO 2009121031 A1 20091001 CAN 151:418165 AN 2009:1194632 CAPLUS

2. McChesney, James D.; Henri, John T.; Venkataraman, Sylesh K.; Lamb, Rodger L.; Foster, Jonathan E.; Sumner, Christian M.; Ye, Shangping; Yiannkouros, George Petros; Stemphoski, Aaron Michael; Walker, Donald G. Processes for the preparation of taxane derivatives and intermediates useful therein. PCT Int. Appl. (2007), 58 pp. CODEN: PIXXD2 WO 2007075870 A2 20070705 CAN 147:143571 AN 2007:728689 CAPLUS

3. Tomillero A; Moral M A Gateways to clinical trials. Methods and findings in experimental and clinical pharmacology (2008), 30(8), 643-72. Journal code: 7909595. ISSN:0379-0355. PubMed ID 19088949 AN 2009036942 MEDLINE

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