RAF-265 (CHIR-265)
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MedKoo CAT#: 200770

CAS#: 405169-16-6

Description: 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. 5).


Price and Availability

Size Price Shipping out time Quantity
10mg USD 190 2 Weeks
25mg USD 350 2 Weeks
50mg USD 550 2 Weeks
100mg USD 950 2 Weeks
200mg USD 1650 2 Weeks
500mg USD 2450 2 Weeks
1g USD 3250 2 Weeks
2g USD 4950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-03-30. Prices are subject to change without notice.

CHIR-265, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 200770
Name: RAF-265 (CHIR-265)
CAS#: 405169-16-6
Chemical Formula: C24H16F6N6O
Exact Mass: 518.12898
Molecular Weight: 518.41
Elemental Analysis: C, 55.60; H, 3.11; F, 21.99; N, 16.21; O, 3.09


Related CAS #: 927880-90-8  

Synonym: CHIR 265; CHIR265; CHIR-265; RAF-265; RAF 265; RAF265.

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

InChi Key: YABJJWZLRMPFSI-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H16F6N6O/c1-36-19-7-6-15(10-17(19)34-22(36)33-14-4-2-13(3-5-14)23(25,26)27)37-16-8-9-31-18(11-16)21-32-12-20(35-21)24(28,29)30/h2-12H,1H3,(H,32,35)(H,33,34)

SMILES Code: FC(C1=CC=C(NC2=NC3=CC(OC4=CC(C5=NC(C(F)(F)F)=CN5)=NC=C4)=CC=C3N2C)C=C1)(F)F


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

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