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。

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Dabrafenib (GSK2118436) 化学構造
分子量: 519.56

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Quality Control & MSDS

製品説明

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    Raf製品生物活性の比較
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製品の説明

生物活性

製品説明 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。
ターゲット 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.
特集

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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)
1

参考

化学情報

Download Dabrafenib (GSK2118436) SDF
分子量 519.56
化学式

C23H20F3N5O2S2

CAS No. 1195765-45-7
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (57.74 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

カスタマーフィードバック (4)


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Source J Clin Invest, 2014, 24(3), 1406-17. Dabrafenib (GSK2118436) purchased from Selleck
Method Western blot
Cell Lines A375P cells
Concentrations 10 uM
Incubation Time 48 h
Results GSK2118436 inhibition produced an additive increase in LC3II/LC3I ratio, but the combination of GSK2118436 with HCQ produced substantial increases in LC3II/LC3I ratio and p62 levels, and the triple drug combination (GSK2118436, GSK1120212, and HCQ) produced the most substantial increase in LC3II/LC3I ratio and buildup of p62, indicative of simultaneous autophagy induction and distal autophagy blockade.

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Source J Clin Invest, 2014, 124(11), 5074-84. Dabrafenib (GSK2118436) purchased from Selleck
Method Western blot
Cell Lines CLL cells
Concentrations 6 uM
Incubation Time 24 h
Results Levels of phosphorylated ERK (pERK) and total ERK (tERK) in enriched CD19+CD5+ CLL cells or CD14+ monocytes were measured by Western blot analysis. CLL cells exposed to dabrafenib or vemurafenib had an elevated pERK/tERK ratio as compared with vehicle(Left). The quantitative results had shown in right(P < 0.01).

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Source Transl Res, 2014, 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.

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Source Cell Death Dis, 2014, 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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