3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide

ChemicalBook > CAS DataBase List > 3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide

3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide

Product Name: 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
Formula Weight: 565.28
MOL File: 874101-00-5.mol

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3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide Property

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

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Safety

Hazard Codes: Xn
Risk Statements: 22
HS Code: 2934999090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 19488
Product name: RO4987655
Packaging: 1mg
Price: $59
Updated: 2024/03/01

Cayman Chemical

Product number: 19488
Product name: RO4987655
Packaging: 5mg
Price: $177
Updated: 2024/03/01

Cayman Chemical

Product number: 19488
Product name: RO4987655
Packaging: 10mg
Price: $266
Updated: 2024/03/01

Cayman Chemical

Product number: 19488
Product name: RO4987655
Packaging: 25mg
Price: $516
Updated: 2024/03/01

Adipogen Life Sciences

Product number: SYN-1188-M005
Product name: CH4987655
Purity: ≥95%
Packaging: 5mg
Price: $535
Updated: 2021/12/16

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3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide Chemical Properties,Usage,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

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874101-00-5, 3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMideRelated Search:

Ro 3306 Bisindoylmaleimide X RO495 3,4-dimethoxy-N-[4-(3-nitrophenyl)-1,3-thiazol-2-yl]benzenesulfonamide ROC-325 RO2959 Hydrochloride (S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((S)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-methylpentanamide

3,4-Difluoro-2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-5-[(3-oxo-2-oxazinanyl)methyl]benzamide

CH4987655(RO4987655)

3,4-difluoro-2-(2-fluoro-4-iodophenylaMino)-N-(2-hydroxyethoxy)-5-((3-oxoMorpholino)Methyl)benzaMide

RO4987655(CH4987655)

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

CH-4987655

CS-1468

RO-4987655; RO 4987655; CH-4987655; CH4987655; CH 4987655

RG7167

Benzamide, 3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-5-[(tetrahydro-3-oxo-2H-1,2-oxazin-2-yl)methyl]-

RO4987655,MAPKK,RO 4987655,CH 4987655,MEK,Mitogen-activated protein kinase kinase,MAP2K,Inhibitor,inhibit,RO-4987655,CH-4987655

874101-00-5

C20H19F3IN3O5