ベムラフェニブ

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H410：長期的影響により水生生物に非常に強い毒性

• 注意書き

  P273：環境への放出を避けること。

  P391：漏出物を回収すること。

  P501：内容物/容器を．．．に廃棄すること。

ベムラフェニブ 化学特性,用途語,生産方法

• 効能

  抗悪性腫瘍薬, BRAFキナーゼ阻害薬

• 商品名

  ゼルボラフ (中外製薬)

• 説明

  In August 2011, the United States FDA approved vemurafenib (PLX- 4032, RO-5185426) for the treatment of patients with metastatic melanoma with the BRAFV600E mutation. Vemurafenib has been developed as a targeted therapy for patients with the BRAF gene mutation since oncogenic B-raf signaling is implicated in approximately 50% of melanomas. Vemurafenib was identified based on an initial high-throughput screen followed by the extensive use of structure-based drug design. Vemurafenib is a potent inhibitor of B-RafV600E kinase (IC₅₀=13 nM) compared to its potency against wildtype B-raf (IC₅₀=160 nM) and is fairly selective versus a panel of 200 kinases. It does inhibit other kinases (RAF1, SRMS, ACK1, MAP4K5, and FGR) and mutant B-raf kinases (BRAFV600K, BRAFV600D, and BRAFV600R) with enzyme IC_50's of <100 nM.

• 化学的特性

  Off-White Solid

• 使用

  Vemurafenib selective BRAFV600E kinase inhibitor; an antitumor agent. Vemurafenib functions by inhibiting the proliferation and mitogen-activated protein/extracellular signal-regulated kinase (ERK) kinase and ERK phosphorylation in a panel of tumor cell lines, including melanoma cell lines expressing BRAFV600E or other mutant BRAF proteins altered at codon 600.

• 定義

  ChEBI: A pyrrolopyridine that is 1H-pyrrolo[2,3-b]pyridine which is substituted at position 5 by a p-chlorophenyl group and at positions 3 by a 3-amino-2,6-difluorobenzoyl group, the amino group of which has undergone ormal condensation with propane-1-sulfonic acid to give the corresponding sulfonamide. An inhibitor of BRAF and other kinases.

ベムラフェニブ 生産企業

Global(246)Suppliers

ベムラフェニブ スペクトルデータ(¹HNMR)

918504-65-1, ベムラフェニブ キーワード