Ulixertinib (BVD-523)

別名：VRT752271

製品コード：S7854 純度：99.99%

Ulixertinib (BVD-523, VRT752271) は、ERK1/ERK2 を強力かつ可逆的に阻害する薬剤であり、ERK2 に対する IC50 は 0.3 nM 未満です。第1相。

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
5mg	JPY 22000	国内在庫あり
25mg	JPY 67000	国内在庫あり
100mg	JPY 149500	国内在庫あり
1g	JPY 220500	国内在庫あり

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文献中Selleckの製品使用例（68）

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

SHP099

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

Ulixertinib (BVD-523)関連製品

関連ターゲット	ERK1 ERK2 ERK5 ERK1/2	もっと見る
関連製品	SCH772984 Ravoxertinib (GDC-0994) LY3214996 (Temuterkib) FR 180204 VX-11e XMD8-92 AZD0364 (ATG-017) ERK5-IN-1 Senkyunolide I Phospho-p44/42 MAPK (Erk1/2) (T202/Y204) Antibody (Rabbit mAb) [D13L13] Astragaloside IV MK-8353 (SCH900353) DEL-22379 KO-947 Magnolin Phospho-Erk1 (T 202/Y 204)/Erk2 (T 185/Y 187) Antibody (Rabbit mAb) [G4M7] Pluripotin (SC1) p44/42 MAPK (Erk1/2) Antibody (Rabbit mAb) [F1E12] ASTX-029 AG-126 CC-90003 BAY-885 Phospho-ERK1/ERK2 (T202/185) Antibody (Rabbit mAb) [G2D16] p44/42 MAPK (Erk1/2) Antibody (Mouse mAb) [E11P7] ERK1 Antibody (Rabbit mAb) [K24F21]	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

ERKシグナル伝達経路

ERK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	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
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

Ulixertinib (BVD-523, VRT752271) は、ERK1/ERK2 を強力かつ可逆的に阻害する薬剤であり、ERK2 に対する IC50 は 0.3 nM 未満です。第1相。

Targets

ERK1	ERK2
	<0.3 nM

In Vitro
In vitro	In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib (BVD-523) 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. It also inhibits A375 cell proliferation with IC50 of 180 nM.
Kinase Assay	ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay
Kinase 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, including Ulixertinib (BVD-523). The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate its 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. Ulixertinib (BVD-523), 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
臨床試験 (data from https://clinicaltrials.gov, updated on 2026-03-12)
NCT05985954	RECRUITING	Metastatic Colorectal Cancer	M.D. Anderson Cancer Center	2024-01-18	PHASE1
NCT03454035	RECRUITING	Tumor, Solid; Pancreatic Cancer; Melanoma	UNC Lineberger Comprehensive Cancer Center	2018-01-30	PHASE1
NCT06773195	RECRUITING	Myelofibrosis	Memorial Sloan Kettering Cancer Center	2025-01-07	PHASE1; PHASE2
NCT05804227	RECRUITING	Gliomas	M.D. Anderson Cancer Center	2023-04-20	EARLY_PHASE1
NCT06411821	RECRUITING	Histiocytic Neoplasms	Memorial Sloan Kettering Cancer Center	2024-05-07	PHASE2
NCT02465060	ACTIVE_NOT_RECRUITING	Advanced Lymphoma; Advanced Malignant Solid Neoplasm; Bladder Carcinoma; Breast Carcinoma; Cervical Carcinoma; Colon Carcinoma; Colorectal Carcinoma; Endometrial Carcinoma; Esophageal Carcinoma; Exocrine Pancreas Carcinoma; Gastric Carcinoma; Glioma; Head and Neck Carcinoma; Hematopoietic and Lymphoid Cell Neoplasm; Kidney Carcinoma; Liver Carcinoma; Lung Carcinoma; Lymphoma; Malignant Uterine Corpus Neoplasm; Malignant Uterine Neoplasm; Melanoma; Multiple Myeloma; Ovarian Carcinoma; Prostate Carcinoma; Rectal Carcinoma; Recurrent Bladder Carcinoma; Recurrent Breast Carcinoma; Recurrent Cervical Carcinoma; Recurrent Colon Carcinoma; Recurrent Colorectal Carcinoma; Recurrent Esophageal Carcinoma; Recurrent Gastric Carcinoma; Recurrent Glioma; Recurrent Head and Neck Carcinoma; Recurrent Liver Carcinoma; Recurrent Lung Carcinoma; Recurrent Lymphoma; Recurrent Malignant Solid Neoplasm; Recurrent Malignant Uterine Corpus Neoplasm; Recurrent Melanoma; Recurrent Multiple Myeloma; Recurrent Ovarian Carcinoma; Recurrent Pancreatic Carcinoma; Recurrent Prostate Carcinoma; Recurrent Rectal Carcinoma; Recurrent Skin Carcinoma; Recurrent Thyroid Gland Carcinoma; Refractory Lymphoma; Refractory Malignant Solid Neoplasm; Refractory Multiple Myeloma; Skin Carcinoma; Thyroid Gland Carcinoma	National Cancer Institute (NCI)	2015-08-17	PHASE2

参考
https://pubmed.ncbi.nlm.nih.gov/25977981/

参考

https://pubmed.ncbi.nlm.nih.gov/25977981/

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

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
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.300mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL 86 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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