规格

价格

库存

数量

1 mg

¥ 549

现货

2 mg

¥ 798

现货

5 mg

¥ 1,280

现货

10 mg

¥ 2,110

现货

25 mg

¥ 3,570

现货

50 mg

¥ 5,160

现货

100 mg

¥ 7,290

现货

500 mg

¥ 14,600

现货

1 mL x 10 mM (in DMSO)

¥ 1,370

现货

生物活性

产品描述	RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.
靶点活性	B-Raf (V600E):8.2 nM, MEK1:160 nM, Raf:56 nM, B-Raf:19 nM
体外活性	在HCT116 KRAS突变型结直肠癌细胞中，CH5126766显著降低了phospho-MEK和phospho-ERK的水平。CH5126766通过与MEK1结合来抑制RAF激酶，使MEK成为RAF的主要负向抑制剂。[1] 在Raf或RAS突变细胞系（包括SK-MEL-28、SK-MEL-2、MIAPaCa-2、SW480、HCT116和PC3细胞）中，CH5126766以分别为65、28、40、46和277 nM的IC50值抑制细胞生长。在携带BRAF V600E或NRAS突变的两个黑色素瘤细胞系中，RO5126766引起G1期细胞周期阻滞，并伴随着CDK抑制剂p27的上调和cyclinD1的下调。[3]
体内活性	在HCT116 (G13D KRAS) 小鼠异种移植模型中，CH5126766 (25 mg/kg, p.o.) 比标准的MEK抑制剂更有效地抑制ERK信号输出，后者诱导MEK磷酸化且具有强大的抗肿瘤活性。[1] 在HCT116 (K-ras) 和COLO205 (B-raf) 突变型异种移植中，CH5126766 (0.3 mg/kg) 显著减少了[18F]FDG摄取。[2] 在SK-MEL-2异种移植模型中，RO5126766同样抑制了肿瘤生长。[3]
激酶实验	MEK and RAF kinase enzyme assays: The inhibitory activities against CRAF, BRAF, or BRAF V600E enzymes are measured by quantification of phosphorylation of inactive K97R MEK1 [MEK1] by recombinant RAF proteins [BRAF: B-RAF wt, BRAF V600E: B-RAF V600E or CRAF: Raf-1] with Europium-anti-MEK1/2 (pSer218/222) antibody and SureLight allophycocyanine-anti-6his antibody by measuring time-resolved fluorescence (TRF). Alternatively, the inhibitory activities against the RAF enzymes are measured by quantification of phosphorylation of a fluorescein-labeled peptide corresponding to human MEK1 212-224 and human MEK2 217-229 (5-Fl-SGQLIDSMANSFV-NH2, MEKtide) by using the IMAP fluorescence polarization (FP) Screening Express Kit. Inhibition of MEK1 is evaluated by a coupled assay with active MEK1 (MEK1 S218E/S222E) and unactive dephosphorylated ERK2 (MAP kinase 2/Erk 2). The phosphorylation of a fluorescent-labeled peptide substrate (FAM-Erktide, IPTTPITTTYFFFK-5FAM-COOH) by ERK2 is quantified by using the IMAP FP Screening Express Kit.
细胞实验	The number of viable cells is determined using the Cell Counting Kit-8 assay according to the manufacturer's instructions. After the incubation of cells for 72 h with the indicated concentrations of various agents, kit reagent WST-8 is added to the medium and incubated for a further 4 h. The absorbance of samples (450 nm) is determined using a scanning multiwell spectrophotometer that serves as an ELISA reader. Cell numbers and viability are also measured using the ViaCount Assay according to the manufacturer's instructions.(Only for Reference)
别名	VS-6766, RO5126766, CH5126766, Avutometinib

化学信息

分子量	471.46
分子式	C₂₁H₁₈FN₅O₅S
CAS No.	946128-88-7
Smiles	CNS(=O)(=O)Nc1nccc(Cc2c(C)c3ccc(Oc4ncccn4)cc3oc2=O)c1F
密度	1.495 g/cm3 (Predicted)

储存&溶解度

存储

溶解度信息

DMSO: 87 mg/mL (184.53 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 5 mg/mL (10.61 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1211 mL	10.6054 mL	21.2107 mL	106.0535 mL
5 mM	0.4242 mL	2.1211 mL	4.2421 mL	21.2107 mL
10 mM	0.2121 mL	1.0605 mL	2.1211 mL	10.6054 mL
20 mM	0.1061 mL	0.5303 mL	1.0605 mL	5.3027 mL
50 mM	0.0424 mL	0.2121 mL	0.4242 mL	2.1211 mL
100 mM	0.0212 mL	0.1061 mL	0.2121 mL	1.0605 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Ro 5126766

Ro 5126766

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

Ro 5126766

Ro 5126766

Ro 5126766 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词