| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Ulixertinib (formerly also known as BVD-523 and VRT752271) is a novel, potent, orally bioactive, highly selective, ATP-competitive, and reversible ERK1/ERK2 inhibitor with potential antineoplastic activity . Its IC50 for inhibiting ERK2 is <0.3 nM. BioMed Valley Discoveries (BVD) is creating ulixertinib to treat myeloid leukemia and myelodysplastic syndrome. Ulixertinib (BVD-523) received an immediate Expanded Access Program (EAP) from the US FDA in September 2020. Myeloma-induced angiogenesis and VEGF secretion by human myeloma cells are inhibited by downregulating ERK protein kinase activity. ERK 1 and 2 are both inhibited by BVD-523 when taken orally, preventing the activation of ERK-mediated signal transduction pathways.
| Targets |
ERK1 ; ERK2 (IC50 = 0.3 nM)
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| ln Vitro |
Ulixertinib lowers the levels of phosphorylated ERK2 (pERK) and phosphorylation of the downstream kinase RSK (pRSK) in the A375 melanoma cell line, which has the b-RAFV600E mutation, with IC50 values of 4.1/0.14 μM, respectively. Additionally, ulixertinib reduces A375 cell proliferation with an IC50 of 180 nM. [1]
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| ln Vivo |
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| Enzyme Assay |
MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are prepared in assay buffer, which is composed of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT, and 0.01% (v/v) CHAPS. A polypropylene, 384-well plate with test and reference control substances is filled with 10 µL of 1.2 nM ERK2 protein that has been prepared in assay buffer. In order to determine the compound IC50s, the compound plates had previously been dosed with a 12-point range from 100 M down to 0.1 nM, with a total DMSO concentration in the assay of 1%. Following a 20-minute pre-incubation period at room temperature, 10 µL of substrate solution—consisting of 16 µM erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer—is added. The addition of 80 µl of 1% (v/v) formic acid quenches the reaction after it has been allowed to proceed for 20 minutes at room temperature. The RapidFire Mass Spectrometry platform is then used to run the assay plates in order to measure the substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
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| Cell Assay |
Cell media containing 10% (v/v) foetal calf serum and 1% (v/v) L-glutamine are used to cultivate A375 cells. Cells are harvested, dispensed into black, 384-well Costar plates with a capacity of 40 L cell media and 200 cells per well, and then incubated overnight at 37 °C, 90% relative humidity, and 5% CO2 in a rotating incubator. Using a Labcyte Echo 555 acoustic dispenser, test substances and reference controls are dosed directly into the cell plates' inner 308 wells. To determine compound IC50s, the cells are dosed over a 12 point range from 30 M to 0.03 nM, with a final DMSO concentration in the assay of 0.3%. The cell plates are then kept at 37°C for the following 72 hours. After 30 minutes of incubation at room temperature, cells were fixed and stained by adding 20 µL of 12% formaldehyde to PBS/A (for a final concentration of 4%), along with a 1:2000 dilution of Hoechst 33342. Using a Cellomics ArrayScanTM VTI imaging platform, a cell count is carried out on the stained cell plates. Additionally, a Day 0 cell plate is fixed, stained, and read to produce a baseline cell count for calculating the compound's cytotoxic and anti-proliferative effects.
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| References |
| Molecular Formula |
C21H22CL2N4O2
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| Molecular Weight |
433.33
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| Exact Mass |
432.11
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| Elemental Analysis |
C, 58.21; H, 5.12; Cl, 16.36; N, 12.93; O, 7.38
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| CAS # |
869886-67-9
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| Related CAS # |
Ulixertinib hydrochloride;1956366-10-1
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| Appearance |
White to off-white solid powder
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| SMILES |
CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)N[C@H](CO)C3=CC(=CC=C3)Cl)Cl
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| InChi Key |
KSERXGMCDHOLSS-LJQANCHMSA-N
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| InChi Code |
InChI=1S/C21H22Cl2N4O2/c1-12(2)26-20-8-16(17(23)10-25-20)14-7-18(24-9-14)21(29)27-19(11-28)13-4-3-5-15(22)6-13/h3-10,12,19,24,28H,11H2,1-2H3,(H,25,26)(H,27,29)/t19-/m1/s1
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| Chemical Name |
N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-chloro-2-(propan-2-ylamino)pyridin-4-yl]-1H-pyrrole-2-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 4.3mg/ml (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03417739 | Active Recruiting |
Drug: BVD-523 | Uveal Melanoma | Dana-Farber Cancer Institute | March 26, 2018 | Phase 2 |
| NCT04488003 | Active Recruiting |
Drug: Ulixertinib Drug: Physician's Choice |
MEK Mutation MEK Alteration |
BioMed Valley Discoveries, Inc | November 3, 2020 | Phase 2 |
| NCT04145297 | Active Recruiting |
Drug: Ulixertinib Drug: Hydroxychloroquine |
Gastrointestinal Neoplasms | University of Utah | March 17, 2020 | Phase 1 |
| NCT03698994 | Active Recruiting |
Drug: Ulixertinib Other: Pharmacokinetic Study |
Recurrent Glioma Refractory Glioma |
National Cancer Institute (NCI) |
October 1, 2018 | Phase 2 |
| NCT05221320 | Recruiting | Drug: Ulixertinib | Tumor, Solid Gastrointestinal Cancer |
BioMed Valley Discoveries, Inc | May 26, 2022 | Phase 2 |
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