3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide
- CAS No.
- 874101-00-5
- Chemical Name:
- 3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide
- Synonyms
- RG7167;CS-1468;CH-4987655;RO4987655(CH4987655);CH4987655(RO4987655);RO-4987655; RO 4987655; CH-4987655; CH4987655; CH 4987655;3,4-Difluoro-2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-5-[(3-oxo-2-oxazinanyl)methyl]benzamide;3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide;2-((2,4-difluorophenyl)aMino)-3,4-difluoro-N-(2-hydroxyethoxy)-5-((3-oxo-1,2-oxazinan-2-yl)Methyl)benzaMide;3,4-Difluoro-2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-5-[(3-oxo-[1,2]oxazinan-2-yl)methyl]benzamide
- CBNumber:
- CB72552593
- Molecular Formula:
- C20H19F3IN3O5
- Molecular Weight:
- 565.28
- MDL Number:
- MFCD19443685
- MOL File:
- 874101-00-5.mol
- MSDS File:
- SDS
3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide Properties
| Density | 1.740±0.06 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | insoluble in H2O; insoluble in EtOH; ≥56.6 mg/mL in DMSO |
| form | solid |
| pka | 14.19±0.10(Predicted) |
| color | White to off-white |
| FDA UNII | I3733P75ML |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501 | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22 | |||||||||
| HS Code | 2934999090 | |||||||||
| NFPA 704 |
|
3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide price More Price(23)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 19488 | RO4987655 | 874101-00-5 | 1mg | $59 | 2024-03-01 | Buy |
| Cayman Chemical | 19488 | RO4987655 | 874101-00-5 | 5mg | $177 | 2024-03-01 | Buy |
| Cayman Chemical | 19488 | RO4987655 | 874101-00-5 | 10mg | $266 | 2024-03-01 | Buy |
| Cayman Chemical | 19488 | RO4987655 | 874101-00-5 | 25mg | $516 | 2024-03-01 | Buy |
| Adipogen Life Sciences | SYN-1188-M005 | CH4987655 ≥95% | 874101-00-5 | 5mg | $535 | 2021-12-16 | Buy |
3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide Chemical Properties,Uses,Production
Biological Activity
ro4987655 is a highly selective and small molecule inhibitor of mek with ic50 value of 5nm [1].ro4987655 is developed with a unique 3-oxo-[1,2]oxazinan-2-ylmethyl group at the 5-position.it is highly selective against mek over other 400 kinases. meanwhile, ro4987655 is a non- competitive inhibitor of mek. it shows higher affinity for mek both in the absence and the presence of atp. ro4987655 has a strong anti-proliferation efficacy in various tumor cells including colo205, ht29, qg56, mia and c32 with ic50 values of 0.86nm, 1.7nm, 9.5nm, 3.3nm and 8.4nm, respectively. in addition, ro4987655 is found to have antitumor activity in a wide range of human cancer xenograft models. in the ht-29 human colon cancer xenograft, ro4987655 shows a strong inhibition of perk formation as well as tumor regression [1, 2].ro4987655 is now in phase i trials. it shows clinical activity in both patients with braf wild-type melanoma and braf v600-mutated melanoma. it is also efficacious in patients with kras-mutated non-small cell lung cancer but not kras-mutated colorectal cancer [2].
References
[1] isshiki y, kohchi y, iikura h, matsubara y, asoh k, murata t, kohchi m, mizuguchi e, tsujii s, hattori k, miura t, yoshimura y, aida s, miwa m, saitoh r, murao n, okabe h, belunis c, janson c, lukacs c, schück v, shimma n. design and synthesis of novel allosteric mek inhibitor ch4987655 as an orally available anticancer agent. bioorg med chem lett. 2011 mar 15;21(6):1795-801.
[2] zimmer l, barlesi f, martinez-garcia m, dieras v, schellens jh, spano jp, middleton mr, calvo e, paz-ares l, larkin j, pacey s, venturi m, kraeber-bodere f, tessier jj, eberhardt we, paques m, guarin e, meresse naegelen v, soria jc. phase i expansion and pharmacodynamic study of the oral mek inhibitor ro4987655 (ch4987655) in selected advanced cancer patients with ras-raf mutations. clin cancer res. 2014 jun 19. pii: clincanres.0341.2014.
3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32836 | 60 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 | |
| Hangzhou Yuhao Chemical Technology Co., Ltd | 0571-82693216 | info@yuhaochemical.com | China | 9394 | 52 |
| Shanghai Topbiochem Technology Co., Ltd | 021-58170097 | info@topbiochem.com | China | 9465 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7553 | 61 |