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Reagents and instruments for immunology, cell biology and molecular biology.

Ulixertinib [869886-67-9]

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Cat# HY-15816-5mg

Size : 5mg

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Brand : MedChemExpress

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Description

Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line^[1]^[2].

IC₅₀ & Target^[2]

ERK2

0.3 nM (IC₅₀, at K_M ATP (60 μM))

ERK1

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.14 μM Compound: BVD-523	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 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	[PMID: 25977981]
A-375	IC₅₀	0.18 μM Compound: BVD-523	Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis	[PMID: 25977981]
A-375	IC₅₀	4.1 μM Compound: BVD-523	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 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	[PMID: 25977981]
ASPC1	IC₅₀	849 nM Compound: BVD523; BVD	Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
BaF3	IC₅₀	2231 nM Compound: BVD523; BVD	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
BaF3	IC₅₀	468 nM Compound: BVD523; BVD	Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
BaF3	IC₅₀	8608 nM Compound: BVD523; BVD	Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay	[PMID: 28038940]
COLO 205	IC₅₀	102.7 nM Compound: BVD-523	Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability for 72 hrs by cell titre glo luminescence assay Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability for 72 hrs by cell titre glo luminescence assay	[PMID: 35450372]
NCI-H23	IC₅₀	1 μM Compound: BVD523; BVD	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
PANC-1	IC₅₀	>1 x 10^-4nM Compound: BVD523; BVD	Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
PANC-1	IC₅₀	>1 x 10^-4nM Compound: BVD523; BVD	Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
PANC-1	IC₅₀	>1 × 10^-4nM Compound: BVD523; BVD	Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
SK-CO-1	IC₅₀	356 nM Compound: BVD523; BVD	Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]
SW-620	IC₅₀	499 nM Compound: BVD523; BVD	Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay	[PMID: 28038940]

In Vitro

Combined Ulixertinib (BVD-523; 10, 20, 30 μM; 48 hours) and VS-5584 treatment causes significant induction of cell death in human pancreatic cancer (HPAC) cells in PDAC cell lines BxPC-3, MIAPaCa-2, and CFPAC-1^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (230.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3077 mL	11.5386 mL	23.0771 mL
5 mM	0.4615 mL	2.3077 mL	4.6154 mL
10 mM	0.2308 mL	1.1539 mL	2.3077 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 1% CMC/saline water
Solubility: 10 mg/mL (23.08 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.95%

Data Sheet (277 KB) SDS (393 KB)

COA (251 KB) HNMR (271 KB) RP-HPLC (242 KB) LCMS (93 KB) Elemental Analysis Report (109 KB)

Handling Instructions (2659 KB)

References

[1]. Ward RA, et al. Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem. 2015 Jun 11;58(11):4790-801. [Content Brief]

[2]. Kumar R, et al. Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. J Pharm Biomed Anal. 2016 Jun 5;125:140-4. [Content Brief]

[3]. Changwen Ning, et al. Targeting ERK Enhances the Cytotoxic Effect of the Novel PI3K and mTOR Dual Inhibitor VS-5584 in Preclinical Models of Pancreatic Cancer. Oncotarget. 2017 Jul 4;8(27):44295-44311. [Content Brief]

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Ulixertinib [869886-67-9]

Cat# HY-15816-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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