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Avutometinib
別名：RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304
Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304) 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.
CAS No. 946128-88-7
文献中Selleckの製品使用例（16）
製品安全説明書
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純度：
99.54%
99.54
Avutometinib関連製品
シグナル伝達経路
Raf阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| human PANC1 cells | Function assay | 10 μM | 1 h | Inhibition of MEK1 in human PANC1 cells assessed as reduction in pErk1/2 level at 10 uM after 1 hr by Western blotting analysis | 25766633 |
| human A549 cells | Function assay | 10 μM | 1 h | Inhibition of MEK1 in human A549 cells assessed as reduction in pErk1/2 level at 10 uM after 1 hr by Western blotting analysis | 25766633 |
| HCT116 cell | Function assay | 96 h | Inhibition of human HCT116 cell growth after 96 hrs by counting kit-8 analysis, IC50=0.04 μM | 24900832 | |
| human C32 cells | Growth inhibition assay | Growth inhibition of human C32 cells harboring R-Raf V600E mutant, IC50=0.047 μM | 24900832 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304) 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. | ||||||||
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| Targets |
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| In Vitro | ||||
| In vitro |
In HCT116 KRAS-mutant colorectal cancer cells, CH5126766 significantly reduces the levels of phospho-MEK and phospho-ERK. CH5126766 inhibits RAF kinase by binding to MEK1, and causes MEK to become a dominant negative inhibitor of RAF. [1] In Raf or RAS-mutant cell lines SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, HCT116, and PC3 cells, CH5126766 inhibits cell growth with IC50 of 65, 28, 40, 46, and 277 nM, respectively. In two melanoma cell lines with the BRAF V600E or NRAS mutation, RO5126766 induces G1 cell cycle arrest accompanied by up-regulation of the CDK inhibitor p27 and down-regulation of cyclinD1. [3] |
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|---|---|---|---|---|
| Kinase Assay | 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). 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. | ||||
| 細胞実験 | 細胞株 | SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, A549, HCT15, HCT116, and PC3 cells | ||
| 濃度 | ~10 μM | |||
| 反応時間 | 72 h | |||
| 実験の流れ | 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. |
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| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-MEKR / MEK / p-ERK / ERK / p27 / ppRB / pRB / Cyclin D1 / Cyclin E |
|
25422890 | |
| In Vivo | ||
| In Vivo |
In an HCT116 (G13D KRAS) mouse xenograft model, CH5126766 (25 mg/kg, p.o.) inhibits ERK signaling output more effectively than a standard MEK inhibitor that induces MEK phosphorylation and has potent antitumor activity. [1] In the HCT116 (K-ras) and COLO205 (B-raf) mutant xenografts, CH5126766 (0.3 mg/kg) causes significant decreases in [18 F]FDG uptake. [2] In the SK-MEL-2 xenograft model, RO5126766 also suppresses the tumor growth. [3] |
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|---|---|---|
| 動物実験 | 動物モデル | Female BALB-nu/nu mice bearing HCT116, Calu-6 or COLO205 tumors |
| 投与量 | ~25 mg/kg | |
| 投与経路 | p.o. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06104488 | Recruiting | Refractory Cancer|CNS Tumors|CNS Tumor Adult|CNS Tumor Childhood|MAP Kinase Family Gene Mutation|NF1|Plexiform Neurofibroma|Low-grade Glioma|Optic Pathway Gliomas|Neuroblastoma|Primary Brain Tumor|Solid Tumor|Solid Tumor Adult|Solid Carcinoma|Central Nervous System Tumor |
Memorial Sloan Kettering Cancer Center |
October 20 2023 | Phase 1 |
| NCT05375994 | Recruiting | Non Small Cell Lung Cancer|KRAS Activating Mutation|Advanced Cancer|Metastatic Cancer|Malignant Neoplasm of Lung|Malignant Neoplastic Disease |
Verastem Inc.|Mirati Therapeutics Inc. |
August 1 2022 | Phase 1|Phase 2 |
化学情報
| 分子量 | 471.46 | 化学式 | C21H18FN5O5S |
| CAS No. | 946128-88-7 | SDF | Download Avutometinib SDFをダウンロードする |
| Smiles | CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F | ||
| 保管 | |||
|
In vitro |
DMSO : 94 mg/mL ( (199.38 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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