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MedKoo product information:

CHIR-265

MedKoo Code#: 200770

Name: CHIR-265

CAS#: 405169-16-6

 

Synonym:  CHIR 265RAF265.

  

IUPAC/Chemical name: 

1-methyl-5-(2-(4-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine

  

Chemical structure: Theoretical analysis

 

 

 Chemical Formula: C24H16F6N6O

Exact Mass: 518.12898

Molecular Weight: 518.41

m/z: 518.12898 (100.0%), 519.13233 (26.0%), 520.13569 (3.2%), 519.12601 (2.2%)

Elemental Analysis: C, 55.60; H, 3.11; F, 21.99; N, 16.21; O, 3.09

 

Availability and price:

This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

Quality control data:

Product will be shipped with supporting analytical data.

 

 

Information about this agent

CHIR-265 is an orally bioavailable small molecule with potential antineoplastic activity.CHIR-265 binds and inhibits Raf kinases, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death. In addition, this agent inhibits vascular endothelial growth factor receptor type 2 (VEGFR-2), thereby disrupting tumor angiogenesis. Raf kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are frequently upregulated in neoplasms. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)


Current developer: Novartis International AG.

 

References

1. Qiu, Zhihui; Li, Shoufeng; Benjamin, Daniel Eliot. Melt granulation process for 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one compound. PCT Int. Appl. (2010), 13 pp. CODEN: PIXXD2 WO 2010003078 A2 20100107 CAN 152:129263 AN 2010:21441

2. Evans, Dean Brent; Jacques, Christian J. Combinations of therapeutic agents comprising vascular disrupting agent such as 5,6-dimethylxanthenone-4-acetic acid, for treating cancer. PCT Int. Appl. (2009), 57pp. CODEN: PIXXD2 WO 2009076170 A2 20090618 CAN 151:86657 AN 2009:739059

3. Rickles, Richard; Lee, Margaret S. Use of adenosine A2A receptor agonists and phosphodiesterase (PDE) inhibitors for the treatment of B-cell proliferative disorders, and combinations with other agents. PCT Int. Appl. (2009), 70 pp. CODEN: PIXXD2 WO 2009011893 A2 20090122 CAN 150:160095 AN 2009:86451

4. Rickles, Richard; Pierce, Laura; Lee, Margaret S. Combinations for the treatment of B-cell proliferative disorders. PCT Int. Appl. (2009), 79pp. CODEN: PIXXD2 WO 2009011897 A1 20090122 CAN 150:160094 AN 2009:83374

5. Renhowe, Paul A.; Pecchi, Sabina; Shafer, Cynthia M.; Machajewski, Timothy D.; Jazan, Elisa M.; Taylor, Clarke; Antonios-McCrea, William; McBride, Christopher M.; Frazier, Kelly; Wiesmann, Marion; Lapointe, Gena R.; Feucht, Paul H.; Warne, Robert L.; Heise, Carla C.; Menezes, Daniel; Aardalen, Kimberly; Ye, Helen; He, Molly; Le, Vincent; Vora, Jayesh; Jansen, Johanna M.; Wernette-Hammond, Mary Ellen; Harris, Alex L. Design, Structure-Activity Relationships and in Vivo Characterization of 4-Amino-3-benzimidazol-2-ylhydroquinolin-2-ones: A Novel Class of Receptor Tyrosine Kinase Inhibitors. Journal of Medicinal Chemistry (2009), 52(2), 278-292. CODEN: JMCMAR ISSN:0022-2623. CAN 150:168237 AN 2009:7206

6. Heise, Carla C.; Hollenbach, Paul; Menezes, Daniel; Pryer, Nancy; Rendahl, Katherine; Wiesmann, Marion. Treatment of melanoma. PCT Int. Appl. (2008), 71pp. CODEN: PIXXD2 WO 2008112509 A1 20080918 CAN 149:370556 AN 2008:1128025

7. Heise, Carla; Masih-Khan, Esther; Moler, Edward; Rowe, Michael; Stewart, Keith; Trudel, Suzanne. Analysis of gene expression profiles in the assessment of the effectiveness of inhibitors FGF receptor 3 in cancer therapy. PCT Int. Appl. (2007), 116pp. CODEN: PIXXD2 WO 2007067968 A2 20070614 CAN 147:46097 AN 2007:643122

8. Chou, Joyce; Okhamafe, Augustus; Frech, Patricia; Gullapalli, Rampurma. Formulations of quinolinones. PCT Int. Appl. (2007), 78pp. CODEN: PIXXD2 WO 2007064719 A2 20070607 CAN 147:16620 AN 2007:619958

9. Chou, Joyce; Gruenke, Larry. Methods for assaying an benzimidazolyl quinoline derivatives in pharmaceutical formulation. PCT Int. Appl. (2007), 35pp. CODEN: PIXXD2 WO 2007056317 A2 20070518 CAN 146:528517 AN 2007:538171

10. Okhamafe, Augustus; Chou, Joyce; Gullapalli, Rampurna; Harwood, Eric; Ryckman, David; Zhu, Shuguang; Shang, Xiao. Crystalline forms of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts. PCT Int. Appl. (2006), 107pp. CODEN: PIXXD2 WO 2006127926 A2 20061130 CAN 146:13206 AN 2006:1252191

11. Michelson, Glenn C.; Chan, Vivien W.; Heise, Carla C.; Wiesmann, Marion; Dawes, Timothy D. Methods for treating drug resistant cancer. PCT Int. Appl. (2006), 151pp. CODEN: PIXXD2 WO 2006124413 A2 20061123 CAN 146:722 AN 2006:1225966

12. Calvin, Gabriel; Harwood, Eric; Ryckman, David; Zhu, Shuguang. Process for preparation of 5-(4-methylpiperazin-1-yl)-2-nitroaniline from 1-methylpiperazine and 5-halo-2-nitroaniline. PCT Int. Appl. (2006), 88pp. CODEN: PIXXD2 WO 2006125130 A1 20061123 CAN 145:505480 AN 2006:1225007

13. Zhu, Shuguang; Harwood, Eric; Cai, Shaopei; Shang, Xiao; Galvin, Gabriel; Jin, Li; Yeung, Arthur; Diaz, Brian; Zheng, Minna; Ryckman, David. The chemical development of CHIR-258. Chimia (2006), 60(9), 584-592. CODEN: CHIMAD ISSN:0009-4293. CAN 147:211781 AN 2006:1141332

14. Lopes De Menezes, Daniel; Heise, Carla; Xin, Xiaohua. Treatment of metastasized tumors. PCT Int. Appl. (2006), 101pp. CODEN: PIXXD2 WO 2006081445 A2 20060803 CAN 145:202872 AN 2006:763835

15. Small, Donald; Whartenby, Katherine A.; Pardoll, Drew. Flt3 inhibitors for immune suppression. PCT Int. Appl. (2006), 81 pp. CODEN: PIXXD2 WO 2006020145 A2 20060223 CAN 144:267266 AN 2006:167710

16. Antonios-McCrea, William R.; Frazier, Kelly A.; Jazan, Elisa M.; Machajewski, Timothy D.; McBride, Christopher M.; Pecchi, Sabina; Renhowe, Paul A.; Shafer, Cynthia M.; Taylor, Clarke. LHMDS mediated tandem acylation-cyclization of 2-aminobenzenecarbonitriles with 2-benzimidazol-2-yl acetates: a short and efficient route to the synthesis of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones. Tetrahedron Letters (2006), 47(5), 657-660. CODEN: TELEAY ISSN:0040-4039. CAN 144:232902 AN 2005:1341902

17. Cai, Shaopei; Chou, Joyce; Harwood, Eric; Heise, Carla C.; Machajewski, Timothy D.; Ryckman, David; Shang, Xiao; Wiesmann, Marion; Zhu, Shuguang. Preparation of benzimidazole quinolinones for inhibiting FGFR3 and treating multiple myeloma. U.S. Pat. Appl. Publ. (2005), 239 pp., Cont.-in-part of U.S. Ser. No. 644,055. CODEN: USXXCO US 2005261307 A1 20051124 CAN 143:477969 AN 2005:1242789

18. Gesner, Thomas G.; Barsanti, Paul A.; Harrison, Stephen D.; Ni, Zhi-Jie; Brammeier, Nathan M.; Zhou, Yasheen; Le, Vincent P. Preparation of benzimidazole quinolinones for inhibiting a checkpoint kinase 1 and their use in combination therapy for cancer. U.S. Pat. Appl. Publ. (2005), 249 pp., Cont.-in-part of U.S. Ser. No. 644,055. CODEN: USXXCO US 2005256157 A1 20051117 CAN 143:477966 AN 2005:1223876

19. Lee, Sang H.; Heise, Carla C. 4-Amino-3-(benzimidazol-2-yl)quinolin-2-one derivatives for the modulation of inflammatory and metastatic processes. PCT Int. Appl. (2005), 145 pp. CODEN: PIXXD2 WO 2005082340 A2 20050909 CAN 143:279443 AN 2005:976928

20. Cai, Shaopei; Chou, Joyce; Harwood, Eric; Heise, Carla C.; Machajewski, Timothy D.; Ryckman, David; Shang, Xiao; Wiesmann, Marion; Zhu, Shuguang. Preparation of benzimidazole quinolinones for inhibiting FGFR3 and treating multiple myeloma. PCT Int. Appl. (2005), 567 pp. CODEN: PIXXD2 WO 2005047244 A2 20050526 CAN 143:7710 AN 2005:451351

21. Cai, Shaopei; Chou, Joyce; Harwood, Eric; Ryckman, David; Shang, Xiao; Zhu, Shuguang; Machajewski, Timothy D. Process for preparation of benzimidazolylquinolones by reaction of aminobenzonitriles with benzimidazolylacetates. PCT Int. Appl. (2005), 77 pp. CODEN: PIXXD2 WO 2005046590 A2 20050526 CAN 143:7732 AN 2005:451119

22. Cai, Shaopei; Chou, Joyce; Harwood, Eric; Machajewski, Timothy D.; Ryckman, David; Shang, Xiao; Zhu, Shuguang. Preparation of benzimidazole quinolinones and lactate salts thereof for inhibiting vascular endothelial growth factor receptor tyrosine kinase. PCT Int. Appl. (2005), 215 pp. CODEN: PIXXD2 WO 2005046589 A2 20050526 CAN 143:7709 AN 2005:451118

23. Machajewski, Timothy D.; Hannah, Alison; Harwood, Eric; Haroldsen, Peter; Heise, Carla C.; Samara, Emil; Shang, Xiao; Vora, Jayesh; Zhu, Shuguang. Methods of treating cancer with a methylpiperazinyl benzimidazolyl quinolinone and related methods. PCT Int. Appl. (2004), 76 pp. CODEN: PIXXD2 WO 2004043389 A2 20040527 CAN 141:1211 AN 2004:428803

24. Barsanti, Paul A.; Bussiere, Dirksen; Harrison, Stephen D.; Heise, Carla C.; Jansen, Johanna M.; Jazan, Elisa; Machajewski, Timothy D.; Mcbride, Christopher; McCrea, William R.; Ng, Simon; Ni, Zhi-Jie; Pecchi, Sabina; Pfister, Keith; Ramurthy, Savithri; Renhowe, Paul A.; Shafer, Cynthia M.; Silver, Joel B.; Wagman, Allan; Weismann, Marion. Preparation of benzimidazole quinolinones for inhibiting a serine/threonine kinase. PCT Int. Appl. (2004), 570 pp. CODEN: PIXXD2 WO 2004018419 A2 20040304 CAN 140:235711 AN 2004:182836

25. Renhowe, Paul A.; Pecchi, Sabina; Machajewski, Timothy D.; Shafer, Cynthia M.; Taylor, Clarke; McCrea, William R.; McBride, Christopher; Jazan, Elisa. Preparation of benzimidazolyl-substituted quinolinone derivatives and analogs, with inhibitory action against vascular endothelial growth factor receptor tyrosine kinase, and useful as anticancer agents. U.S. Pat. Appl. Publ. (2003), 69 pp., Cont.-in-part of U.S. Pat. Appl. 2002 107,392. CODEN: USXXCO US 2003028018 A1 20030206 CAN 138:153534 AN 2003:98039

26. Renhowe, Paul; Pecchi, Sabina; Machajewski, Tim; Shafer, Cynthia; Taylor, Clarke; McCrea, Bill; McBride, Chris; Jazan, Elisa; Wernette-Hammond, Mary-Ellen; Harris, Alex. Benzimidazolyl-substituted quinolinone derivatives and analogs, with inhibitory action against vascular endothelial growth factor receptor tyrosine kinase, and useful as anticancer agents. PCT Int. Appl. (2002), 207 pp. CODEN: PIXXD2 WO 2002022598 A1 20020321 CAN 136:263158 AN 2002:220574  

 

 

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