Avutometinib(别名:RO-5126766、CH-5126766)是一种正在开发的 Ras-Raf-MEK-ERK 信号传导抑制剂。Avutometinib能强力抑制MEK1/2激酶活性并诱导形成显性负性RAF/MEK复合物,从而阻断RAF对MEK的代偿性激活。
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Name | Avutometinib ( 别名: Ro 5126766; CH5126766 ) |
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Iupac Chemical Name | 3-[[3-fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one |
Synonyms | Ro5126766 ; Ro 5126766 ; CH-5126766 ; CH5126766 ; CH 5126766 ; CKI-27 ;R-7304 ;RG-7304 ; VS-6766 |
Molecular Formula | C21H18FN5O5S |
Molecular Weight | 471.462 |
Smile | CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F |
InChiKey | LMMJFBMMJUMSJS-UHFFFAOYSA-N |
InChi | InChI=1S/C21H18FN5O5S/c1-12-15-5-4-14(31-21-25-7-3-8-26-21)11-17(15)32-20(28)16(12)10-13-6-9-24-19(18(13)22)27-33(29,30)23-2/h3-9,11,23H,10H2,1-2H3,(H,24,27) |
CAS Number | 946128-88-7 |
Related CAS | 946128-88-7 |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | 固体粉末 |
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Purity | ≧98.0% |
Storage | 0-4℃,可保存几天到几周;-20℃,可保存 几个月。 |
Solubility | 溶于DMSO (DMSO : ≥ 100 mg/mL) |
Handling | Refer to MSDS |
Shipping Condition | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
HS Code | 2934200090 |
Targets | RAF/MEK抑制剂 |
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Mechanism | Avutometinib是一种RAF/MEK抑制剂,它能够诱导MEK与ARAF、BRAF和CRAF形成非活性复合物,可能通过最大程度地抑制RAS信号通路产生更全面和持久的抗肿瘤反应。与其他MEK抑制剂不同,avutometinib既能阻止MEK激酶活性,也能阻止RAF磷酸化MEK。这种独特的机制使avutometinib能够阻止MEK信号,而不触发补偿性的MEK激活。 |
Cell study | |
Animal study | |
Clinical study |