Dabrafenib (GSK2118436)

Dabrafenib(GSK2118436)は、B-Rafの強力なATP競争的阻害剤で、 B-Raf、 B-RafV600E 、c-Rafに作用する時、 IC50 がそれぞれ 3.2 nM、 0.8 nM 、 5.0 nMです。

5 5 2レビュー 5製品表彰状
価格 在庫  
USD 113 In stock
USD 163 In stock
USD 214 In stock
USD 226 In stock
USD 340 In stock
USD 504 In stock

Dabrafenib (GSK2118436) 化学構造
分子量: 519.56



Quality Control & MSDS


  • Compare Raf Inhibitors
  • 研究分野
  • Combination Therapy



情報 Dabrafenib(GSK2118436)は、B-Rafの強力なATP競争的阻害剤で、 B-Raf、 B-RafV600E 、c-Rafに作用する時、 IC50 がそれぞれ 3.2 nM、 0.8 nM 、 5.0 nMです。
目標 B-raf B-RafV600E c-Raf
IC50 3.2 nM 0.8 nM 5.0 nM [1]
In vitro試験 Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-RafV600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-RafV600E. [1]
In vivo試験 Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. [1]
臨床試験 Dabrafenib is currently in phase 3 clinical trial in patients with melanoma.

推薦された実験操作 (公開の文献だけ)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.
Body Surface Area (m2)
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Dabrafenib (GSK2118436) SDF
分子量 519.56


CAS No. 1195765-45-7
保管 2年-20℃
6月-80℃in DMSO
溶解度 (25°C) * In vitro DMSO 30 mg/mL (57 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 8 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide


カスタマーレビュー (2)

Click to enlarge
Source Cell Death Dis, 2014, 5, 5:e1278. Dabrafenib (GSK2118436) purchased from Selleck
Method TUNEL staining
Cell Lines C57Bl/6J mice
Concentrations 100/300 mg/kg
Incubation Time 1 h
Results Dabrafenib protects mice from acetaminophen-induced hepatotoxicity.The pretreatment of mice with dabrafenib (100 mg/kg or 300 mg/kg) apparently eased the acetaminophen-caused liver injury.

Click to enlarge
Source Transl Res, 2014, 23: 10.1016/j.trsl.2014.06.005. Dabrafenib (GSK2118436) purchased from Selleck
Method MTT assay
Cell Lines FRO and SW1736 cells
Concentrations 0-5 uM
Incubation Time 72 h
Results Dabrafenib showed inhibition of cell growth with concentrations between 0.5 and 5 uM.

製品表彰状 (5)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related Raf 阻害剤

  • Encorafenib (LGX818)

    Encorafenib (LGX818) is a potent and selective BRAFV600E kinase inhibitor with IC50 of 0.3 nM.

  • TAK-632

    TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

  • Sorafenib

    Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

  • FR 180204

    FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively.

  • Vemurafenib (PLX4032, RG7204)

    Vemurafenib (PLX4032, RG7204)新しくて強力な阻害剤で、 B-RAFV600Eに作用すると、IC50 が 31 nMになる。

    Features:PLX4032是新型有效的B-RAFV600E 肿瘤蛋白抑制剂。

  • Sorafenib Tosylate

    Sorafenib Tosylateは、Raf-1、B-RafとVEGFR-2のマルチキナーゼ阻害剤で、IC50 がそれぞれ 6 nM、 22 nM、90 nMです。

  • PLX-4720

    PLX-4720は、B-Raf(V600E)とc-Raf-1(Y340D/Y341D)の「実行中の」形の強力で選択的な阻害剤で、IC50 がそれぞれ 13 nM と 6.7 nMです。

  • SB590885


    Features:SB590885 displays significant selectivity for B-Raf over c-Raf.

  • AZ 628

    AZ 628は力なチロシン・タンパク質阻害剤、 野生のタイプCRAFと BRAF V600Eに作用すると、 IC50 がそれぞれ 29 nM と 34 nMになる。


Tags: Dabrafenib (GSK2118436)を買う | Dabrafenib (GSK2118436)供給者 | Dabrafenib (GSK2118436)を購入する | Dabrafenib (GSK2118436)費用 | Dabrafenib (GSK2118436)生産者 | オーダーDabrafenib (GSK2118436) | Dabrafenib (GSK2118436)代理店