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).


Chemical Structure

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RAF-265 (CHIR-265)
CAS# 405169-16-6

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

Price and Availability

Size Price Availability Quantity
10.0mg USD 190.0 2 Weeks
25.0mg USD 350.0 2 Weeks
50.0mg USD 550.0 2 Weeks
100.0mg USD 950.0 2 Weeks
200.0mg USD 1650.0 2 Weeks
500.0mg USD 2450.0 2 Weeks
1.0g USD 3250.0 2 Weeks
2.0g USD 4950.0 2 Weeks
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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

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

Preparing Stock Solutions

The following data is based on the product molecular weight 518.41 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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



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.