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抑制剂/激活剂

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凋亡与自噬

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Binimetinib (MEK162)

Binimetinib (MEK162) MEK162; ARRY-162; ARRY-438162

Binimetinib (MEK162, ARRY-162, ARRY-438162)是一种有效的MEK1/2抑制剂，无细胞试验中IC50为12 nM。Binimetinib可在人类NSCLC细胞系中诱导G1细胞周期阻滞和凋亡，并诱导自噬。Phase 3。

货号：
TK0380
规格：

1mg

5mg

10mg

50mg

100mg
价格：
￥0.00

产品参数

CAS No.	606143-89-9
生物活性	Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
分子式	C17H15BrF2N4O3
分子量	441.23
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (113.32 mM; Need ultrasonic)
体外研究	In MCF7 cells, RSK3 or RSK4 expression decreases response to treatment with any of the PI3K inhibitors alone. However, the combination of PI3K inhibition with Binimetinib (MEK162) or BI-D1870 completely reverses the resistance of RSK-expressing cells. Binimetinib (MEK162) blocks basal ERK phosphorylation in all HRAS mutant cell lines. The combination of RAD001 and AZD6244/MEK162 causes a stronger inhibition of S6 kinase than single use of RAD001 on Western blot. The combination of RAD001 and AZD6244/MEK162 also translated in a stronger blockade of cell growth in HRAS mutant cells than single use. Binimetinib (MEK162) shows stronger synergism with RAD001 than AZD6244.
文献	•Cancer Cell. 2020 Mar 16;37(3):387-402.e7. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Neuro Oncol. 2019 Mar 18;21(4):486-497. •Oncogene. 2016 Jun 9;35(23):2961-70. •Cancer Lett. 2020 Apr 10;475:53-64. •Cell Syst. 2020 Nov 18;11(5):478-494.e9. •Sci Signal. 2018 Oct 30;11(554):eaar6795. •Comput Struct Biotechnol J. 2019 Feb 8;17:352-361. •Molecules. 2021 May 5;26(9):2717. •Chem Res Toxicol. 2021 Mar 17. •Pigment Cell Melanoma Res. 2017 Sep;30(5):467-476. •Bioanalysis. 2022 Jan;14(2):75-86. •bioRxiv. 2019 Sep. •Patent. US20180263995A1. •Oncotarget. 2017 May 30;8(47):82027-82036. •Oncotarget. 2017 Feb 28;8(9):14835-14846. •Oncotarget. 2016 Apr 12;7(15):19997-20015.
纯度及产品资料	98%

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