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Ulixertinib

Catalog No. T7005 CAS 869886-67-9

Synonyms: BVD-523, VRT752271

Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1/ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.

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Ulixertinib, CAS 869886-67-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 143.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 372.00
200 mg	In stock	$ 538.00
500 mg	In stock	$ 857.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.95%

Purity: 99.89%

Purity: 99.66%

Purity: 99.41%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1/ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.
Targets&IC50	ERK2:<0.3 nM
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.
Cell Research	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.(Only for Reference)

Synonyms	BVD-523, VRT752271
Molecular Weight	433.33
Formula	C21H22Cl2N4O2
CAS No.	869886-67-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

DMSO: 80 mg/mL (184.6 mM)

Ethanol: 12 mg/mL (27.7 mM)

References and Literature

1. Ward RA, et al. J Med Chem. 2015, 58(11), 4790-4801. 2. Caiola E, Iezzi A, Tomanelli M, et al. LKB1 deficiency renders non-small-cell lung cancer cells sensitive to ERK inhibitors.: ERK inhibitors in LKB1 mutated NSCLC[J]. Journal of Thoracic Oncology. 2019.

Citations

1. Caiola E, Iezzi A, Tomanelli M, et al. LKB1 deficiency renders non-small-cell lung cancer cells sensitive to ERK inhibitors.: ERK inhibitors in LKB1 mutated NSCLC. Journal of Thoracic Oncology. 2019 2. Caiola E, Iezzi A, Tomanelli M, et al. LKB1 Deficiency Renders NSCLC Cells Sensitive to ERK Inhibitors. Journal of Thoracic Oncology. 2020, 15(3): 360-370

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Target-Focused Phenotypic Screening Library Covalent Inhibitor Library Clinical Compound Library Anti-Aging Compound Library

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Keywords

Ulixertinib 869886-67-9 MAPK ERK VRT 752271 inhibit BVD 523 BVD-523 VRT-752271 BVD523 Inhibitor VRT752271 Extracellular signal regulated kinases inhibitor

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