Ulixertinib (BVD-523)

別名:VRT752271

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Ulixertinib (BVD-523)化学構造

CAS No. 869886-67-9

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 34000 国内在庫あり
JPY 22000 国内在庫あり
JPY 67000 国内在庫あり
JPY 149500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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製品安全説明書

現在のバッチを見る: 純度: 99.99%
99.99

Ulixertinib (BVD-523)と併用されることが多い化合物

Encorafenib


Ulixertinib, Encorafenib, and Cetuximab combo inhibits tumor growth better in CRC with BRAFV600E mutations.

Knoerzer D, et al. Cancer Res (2023) 83 (7_Supplement): 2693.

SHP099


Ulixertinib and SHP099 inhibit downstream MAPK signaling in SK-N-AS and CHP-212 cells and result in tumor growth delay in xenograft mice model.

Valencia-Sama I, et al. Cancer Res. 2020 Aug 15;80(16):3413-3423.

Trametinib (GSK1120212)


Ulixertinib and Trametinib plus Trastuzumab deruxtecan are extremely effective and lead to complete tumor regression in all PDX models.

Bulle AS, et al. Cancer Res (2022) 82 (12_Supplement): 5333.

Palbociclib


Ulixertinib and Palbociclib exhibit significant inhibition of tumor growth in the MB1998 patient-derived xenograft (PDX) model.

Nassar KW, et al. Mol Cancer Ther. 2021 Oct;20(10):2049-2060.

Gemcitabine


Ulixertinib enhances Gemcitabine's pro-apoptotic effect in HPNE-KRAS G12D cells, effectively inhibiting tumor growth in MIA Paca-2 xenografts.

Jiang H, et al. Mol Cancer Ther. 2018 Oct;17(10):2144-2155.

Ulixertinib (BVD-523)関連製品

シグナル伝達経路

ERK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
A375 Function assay 2 hrs Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 0.14 μM. 25977981
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 0.18 μM. 25977981
SKCO1 Antiproliferative assay 72 hrs Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.356 μM. 28038940
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.468 μM. 28038940
SW620 Antiproliferative assay 72 hrs Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.499 μM. 28038940
AsPC1 Antiproliferative assay 72 hrs Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.849 μM. 28038940
NCI-H23 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay, IC50 = 1 μM. 28038940
SW156 Antiproliferative assay 72 hrs Antiproliferative activity against human SW156 cells harboring wild type KRAS after 72 hrs by CellTiter-Glo assay, IC50 = 1.24 μM. 28038940
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay, IC50 = 2.231 μM. 28038940
A375 Function assay 2 hrs Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 4.1 μM. 25977981
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay, IC50 = 8.608 μM. 28038940
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated RSK levels, IC50 = 0.031 μM. 28376306
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated ERK2 levels, IC50 = 4.1 μM. 28376306
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生物活性

製品説明 Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Targets
ERK1 [1] ERK2 [1]
<0.3 nM
In Vitro
In vitro In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1]
Kinase Assay ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay
MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
細胞実験 細胞株 A375 cells
濃度 ~30 μM
反応時間 72 h
実験の流れ A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-ERK / ERK / RRM2 28797284
Growth inhibition assay Cell viability 30771617
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04488003 Active not recruiting
Advanced Solid Tumor|BRAF Gene Mutation|BRAF Gene Alteration|MEK Mutation|MEK Alteration|MAP2K1 Gene Mutation|MAP2K1 Gene Alteration|MAP2K2 Gene Mutation|MAP2K2 Gene Alteration
BioMed Valley Discoveries Inc
November 3 2020 Phase 2
NCT04145297 Active not recruiting
Gastrointestinal Neoplasms
University of Utah|BioMed Valley Discoveries Inc
March 17 2020 Phase 1
NCT03698994 Active not recruiting
Advanced Malignant Solid Neoplasm|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Primary Malignant Central Nervous System Neoplasm|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Primary Malignant Central Nervous System Neoplasm|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor
National Cancer Institute (NCI)
November 14 2018 Phase 2
NCT03417739 Active not recruiting
Uveal Melanoma
Dana-Farber Cancer Institute|BioMed Valley Discoveries Inc
March 26 2018 Phase 2
NCT02994732 Completed
Healthy
BioMed Valley Discoveries Inc
January 2017 Phase 1

化学情報

分子量 433.33 化学式

C21H22Cl2N4O2

CAS No. 869886-67-9 SDF Download Ulixertinib (BVD-523) SDFをダウンロードする
Smiles CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl
保管

In vitro
Batch:

DMSO : 86 mg/mL ( (198.46 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。)

Ethanol : 86 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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

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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