Ulixertinib hydrochloride
Based on 52 publication(s) in Google Scholar
Ulixertinib hydrochloride (BVD-523 hydrochloride) 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 hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.89%
- No. CAS: 1956366-10-1
- Fòrmula: C21H23Cl3N4O2
- Peso molecular:469.79
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ulixertinib hydrochloride
More- Signal Transduct Target Ther. 2026 Apr 8;11(1):125. [Abstract]
- Nature. 2026 Apr;652(8110):740-751. [Abstract]
- Cancer Res. 2024 Jun 14;84(12):1963-1977. [Abstract]
- Nat Commun. 2023 Nov 2;14(1):6997. [Abstract]
- Nat Commun. 2023 May 19;14(1):2859. [Abstract]
- Nat Commun. 2022 Jul 14;13(1):4078. [Abstract]
- Sci Transl Med. 2021 Jan 27;13(578):eaba7308. [Abstract]
- Theranostics. 2022 Oct 3;12(16):7051-7066. [Abstract]
- Adv Sci (Weinh). 2026 May 26:e15158. [Abstract]
- Adv Sci (Weinh). 2025 Jan;12(2):e2407662. [Abstract]
- Adv Sci (Weinh). 2022 Oct;9(30):e2200717. [Abstract]
- Cell Rep Med. 2025 Feb 18;6(2):101970. [Abstract]
- Sci Adv. 2026 May 8;12(19):eadz0196. [Abstract]
- Sci Adv. 2023 Nov 15;9(46):eadi5921. [Abstract]
- Cell Death Differ. 2024 Jun;31(6):804-819. [Abstract]
- Pharmacol Res. 2023 Nov:197:106955. [Abstract]
- Cancer Lett. 2025 Feb 1:610:217339. [Abstract]
- Cell Death Discov. 2022 Aug 17;8(1):365. [Abstract]
- J Transl Med. 2025 Feb 28;23(1):244. [Abstract]
- Dev Cell. 2020 Sep 14;54(5):608-623.e5. [Abstract]
- Phytother Res. 2026 Apr 27. [Abstract]
- Cell Rep. 2026 Jan 22;45(2):116903. [Abstract]
- Cell Rep. 2021 Dec 28;37(13):110174. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- J Invest Dermatol. 2021 Apr;141(4):852-862.e6. [Abstract]
- J Ethnopharmacol. 2026 Oct 28:369:121888. [Abstract]
- Biochem Pharmacol. 2026 Mar:245:117656. [Abstract]
- Life Sci. 2025 May 15:369:123553. [Abstract]
- Matrix Biol. 2022 Sep:112:20-38. [Abstract]
- Mar Drugs. 2026 Feb 5;24(2):69. [Abstract]
- J Gastroenterol. 2024 Jul;59(7):629-640. [Abstract]
- Cancer Biol Ther. 2022 Dec 31;23(1):69-82. [Abstract]
- Cancer. 2020 Mar 15;126(6):1339-1350. [Abstract]
- Front Cell Dev Biol. 2018 Sep 25:6:111. [Abstract]
- Sci Rep. 2025 Jul 1;15(1):21328. [Abstract]
- Neoplasia. 2025 Jan:59:101085. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- Cancers (Basel). 2022 Feb 14;14(4):954. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Ren Fail. 2025 Dec;47(1):2580064. [Abstract]
- Innate Immun. 2020 Aug;26(6):505-513. [Abstract]
- Mol Cell Endocrinol. 2024 Mar 1:582:112140. [Abstract]
- Platelets. 2024 Dec;35(1):2354833. [Abstract]
- Biomed Chromatogr. 2020 Oct;34(10):e4923. [Abstract]
- Charles University. 2026.
- bioRxiv. 2025 Dec 5.
- bioRxiv. 2025 Dec 27.
- bioRxiv. 2025 Mar 28:2025.03.25.645097. [Abstract]
- Research Square Preprint. 2024 Nov 26.
- Research Square Print. 2023 Feb 22.
- Ulm University. 2021 Mar.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
Customer Validation & Images
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IHC
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WB
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WB
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
Actividad biológica
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.
Chemical Information
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No. CAS 1956366-10-1
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Appearance Solid
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Peso molecular 469.79
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Fòrmula C21H23Cl3N4O2
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC(NC(C)C)=NC=C2Cl)=CN1)N[C@@H](C3=CC=CC(Cl)=C3)CO.[H]Cl
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Synonyms
BVD-523 hydrochloride; VRT752271 hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (52)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
BMX inhibition overcomes small cell lung cancer chemoresistance by stabilizing E2F1 via ERK1/2-Cyclin D1/CDK4/6 axis. [Abstract]2026 Apr 8;11(1):125. PMID: 41946708 -
Nature
2026 Apr;652(8110):740-751. PMID: 41741641 -
Cancer Res
Oncogenic KRAS induces arginine auxotrophy and confers a therapeutic vulnerability to SLC7A1 inhibition in non-small cell lung cancer. [Abstract]2024 Jun 14;84(12):1963-1977. PMID: 38502865 -
Nat Commun
Toxic PARP trapping upon cAMP-induced DNA damage reinstates the efficacy of endocrine therapy and CDK4/6 inhibitors in treatment-refractory ER+ breast cancer. [Abstract]2023 Nov 2;14(1):6997. PMID: 37914699
Ulixertinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Nov 2;14(1):6997. [Abstract]
Western blot analyses in MCF-7 cells treated with tamoxifen, GebR-7b or the ERK inhibitor, Ulixertinib for 20 min or 24 hours in combination with E2.
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Nat Commun
ERK and USP5 govern PD-1 homeostasis via deubiquitination to modulate tumor immunotherapy. [Abstract]2023 May 19;14(1):2859. PMID: 37208329
Ulixertinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 19;14(1):2859. [Abstract]
IB analysis of WCL and GST pull-down precipitates from HEK293T cell lysates with ectopic expression of PD-1-cHA incubated with recombinant GST-USP5 protein. Cells were treated with 1 μM Ulixertinib for 24 h.
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Nat Commun
HRS phosphorylation drives immunosuppressive exosome secretion and restricts CD8+ T-cell infiltration into tumors. [Abstract]2022 Jul 14;13(1):4078. PMID: 35835783
Ulixertinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jul 14;13(1):4078. [Abstract]
Transwells were pretreated with fibronectin and sEVs from B16F10 cells with or without BVD-523 (2 μM; 24 h). Percentages of transmigrated mouse CD8+ T cells induced by CXCL9 were accessed.
Ulixertinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jul 14;13(1):4078. [Abstract]
Growth of B16F10 tumors expressing HRSWT, HRSS345A, or HRSS345D treated with vehicle, anti-PD-1, BVD-523 (BVD), or anti-PD-1 plus BVD-523 (50 mg/kg; p.o. twice daily) as indicated.
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Sci Transl Med
A chimeric antigen receptor with antigen-independent OX40 signaling mediates potent antitumor activity. [Abstract]2021 Jan 27;13(578):eaba7308. PMID: 33504651 -
Theranostics
ERK inactivation enhances stemness of NSCLC cells via promoting Slug-mediated epithelial-to-mesenchymal transition. [Abstract]2022 Oct 3;12(16):7051-7066. PMID: 36276640 -
Adv Sci (Weinh)
Genome-Wide CRISPR Screen Identifies a microRNA Orchestrating Pleiotropic Resistance to Targeted Therapy and T Cell Immunity in Melanoma. [Abstract]2026 May 26:e15158. PMID: 42189126 -
Adv Sci (Weinh)
Osteoblast-Derived ECM1 Promotes Anti-Androgen Resistance in Bone Metastatic Prostate Cancer. [Abstract]2025 Jan;12(2):e2407662. PMID: 39563492 -
Adv Sci (Weinh)
Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. [Abstract]2022 Oct;9(30):e2200717. PMID: 36045417 -
Cell Rep Med
2025 Feb 18;6(2):101970. PMID: 39938523 -
Sci Adv
RAB5c orchestrates LC3-associated phagocytosis to promote microbicidal function of macrophages. [Abstract]2026 May 8;12(19):eadz0196. PMID: 42102192 -
Sci Adv
The SMYD3-MAP3K2 signaling axis promotes tumor aggressiveness and metastasis in prostate cancer. [Abstract]2023 Nov 15;9(46):eadi5921. PMID: 37976356 -
Cell Death Differ
Differential contribution for ERK1 and ERK2 kinases in BRAFV600E-triggered phenotypes in adult mouse models. [Abstract]2024 Jun;31(6):804-819. PMID: 38698060
Ulixertinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Jun;31(6):804-819. [Abstract]
Representative images and quantifications showing CD45R, CD8, CD4, and FOXP3 immunostainings in lung sections of TMX-administered Erk and Erk;BRAFV600E mice treated with Ulixertinib (200 mg/kg/day; p.o. twice a day).
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Pharmacol Res
Tetrandrine synergizes with MAPK inhibitors in treating KRAS-mutant pancreatic ductal adenocarcinoma via collaboratively modulating the TRAIL-death receptor axis. [Abstract]2023 Nov:197:106955. PMID: 37820855 -
Cancer Lett
Chemoresistance-motility signature of molecular evolution to chemotherapy in non-muscle-invasive bladder cancer and its clinical implications. [Abstract]2025 Feb 1:610:217339. PMID: 39608442 -
Cell Death Discov
Ribosomal protein L22-like1 (RPL22L1) mediates sorafenib sensitivity via ERK in hepatocellular carcinoma. [Abstract]2022 Aug 17;8(1):365. PMID: 35973992 -
J Transl Med
RPL22L1 fosters malignant features of cervical cancer via the modulation of DUSP6-ERK axis. [Abstract]2025 Feb 28;23(1):244. PMID: 40022129 -
Dev Cell
An Excitable Ras/PI3K/ERK Signaling Network Controls Migration and Oncogenic Transformation in Epithelial Cells. [Abstract]2020 Sep 14;54(5):608-623.e5. PMID: 32877650 -
Phytother Res
(+)-Matairesinol, Derived From Olive Oil, Enhanced T-Cell Anti-Tumor Immune via JAK3-STAT1 Signal and Synergized With Anti-PD-1 Efficacy. [Abstract]2026 Apr 27. PMID: 42037203 -
Cell Rep
A shear stress-responsive pathway in monocytes drives cardiopulmonary bypass-induced inflammation via spectrin/RAF1/store-operated calcium entry. [Abstract]2026 Jan 22;45(2):116903. PMID: 41579376 -
Cell Rep
2021 Dec 28;37(13):110174. PMID: 34965422 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Invest Dermatol
Inhibition of the Extracellular Signal-Regulated Kinase/Ribosomal S6 Kinase Cascade Limits Chlamydia trachomatis Infection. [Abstract]2021 Apr;141(4):852-862.e6. PMID: 32918951 -
J Ethnopharmacol
"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]2026 Oct 28:369:121888. PMID: 42202911 -
Biochem Pharmacol
IL-18 potentiates platelet activation and thrombosis through IL-18Rα-dependent MAPKs and PI3K/Akt signaling. [Abstract]2026 Mar:245:117656. PMID: 41421453 -
Life Sci
Polymyxin B induces pigmentation by upregulating ATG2A-ERK/CREB-MITF-PMEL17 signaling axis. [Abstract]2025 May 15:369:123553. PMID: 40074142 -
Matrix Biol
2022 Sep:112:20-38. PMID: 35940338 -
Mar Drugs
Anti-Inflammatory Effects of Marine-Derived Resorcylic Acid Lactone Derivatives in Ulcerative Colitis via the MAPK/ERK Pathway. [Abstract]2026 Feb 5;24(2):69. PMID: 41745472 -
J Gastroenterol
Patient-derived organoids of pancreatic ductal adenocarcinoma for subtype determination and clinical outcome prediction. [Abstract]2024 Jul;59(7):629-640. PMID: 38684511 -
Cancer Biol Ther
Repeated treatments of Capan-1 cells with PARP1 and Chk1 inhibitors promote drug resistance, migration and invasion. [Abstract]2022 Dec 31;23(1):69-82. PMID: 35000525 -
Cancer
ERK inhibition effectively overcomes acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib. [Abstract]2020 Mar 15;126(6):1339-1350. PMID: 31821539 -
Front Cell Dev Biol
Fast Dynamic in vivo Monitoring of Erk Activity at Single Cell Resolution in DREKA Zebrafish. [Abstract]2018 Sep 25:6:111. PMID: 30320107 -
Sci Rep
2025 Jul 1;15(1):21328. PMID: 40596490 -
Neoplasia
Ovulation sources ROS to confer mutagenic activities on the TP53 gene in the fallopian tube epithelium. [Abstract]2025 Jan:59:101085. PMID: 39637685 -
Cancers (Basel)
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]2022 Mar 19;14(6):1575. PMID: 35326726 -
Cancers (Basel)
Hyperactivation of MAPK Induces Tamoxifen Resistance in SPRED2-Deficient ERα-Positive Breast Cancer. [Abstract]2022 Feb 14;14(4):954. PMID: 35205702 -
J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
Ren Fail
A multi-omics landscape of programmed cell death in acetaminophen-induced acute kidney injury. [Abstract]2025 Dec;47(1):2580064. PMID: 41249093 -
Innate Immun
IL-33/ST2 axis promotes the inflammatory response of nasal mucosal epithelial cells through inducing the ERK1/2 pathway. [Abstract]2020 Aug;26(6):505-513. PMID: 32456598
Ulixertinib hydrochloride purchased from MedChemExpress. Usage Cited in: Innate Immun. 2020 Aug;26(6):505-513. [Abstract]
The protein levels of p-ERK1/2, ERK1/2, p-RSK, and RSK are measured by Western blotting.
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Mol Cell Endocrinol
Metformin inhibits cell proliferation and ACTH secretion in AtT20 cells via regulating the MAPK pathway. [Abstract]2024 Mar 1:582:112140. PMID: 38147953 -
Platelets
Application of the Cellular Thermal Shift Assay (CETSA) to validate drug target engagement in platelets. [Abstract]2024 Dec;35(1):2354833. PMID: 38767506 -
Biomed Chromatogr
2020 Oct;34(10):e4923. PMID: 32558944 -
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bioRxiv
RAB5c controls the assembly of non-canonical autophagy machinery to promote phagosome maturation and microbicidal function of macrophages. [Abstract]2025 Mar 28:2025.03.25.645097. PMID: 40196584 -
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ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
Solvente y solubilidad
DMSO : 100 mg/mL (212.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. 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]
[2]. 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]
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1286 mL | 10.6431 mL | 21.2861 mL | 53.2153 mL |
| 5 mM | 0.4257 mL | 2.1286 mL | 4.2572 mL | 10.6431 mL | |
| 10 mM | 0.2129 mL | 1.0643 mL | 2.1286 mL | 5.3215 mL | |
| 15 mM | 0.1419 mL | 0.7095 mL | 1.4191 mL | 3.5477 mL | |
| 20 mM | 0.1064 mL | 0.5322 mL | 1.0643 mL | 2.6608 mL | |
| 25 mM | 0.0851 mL | 0.4257 mL | 0.8514 mL | 2.1286 mL | |
| 30 mM | 0.0710 mL | 0.3548 mL | 0.7095 mL | 1.7738 mL | |
| 40 mM | 0.0532 mL | 0.2661 mL | 0.5322 mL | 1.3304 mL | |
| 50 mM | 0.0426 mL | 0.2129 mL | 0.4257 mL | 1.0643 mL | |
| 60 mM | 0.0355 mL | 0.1774 mL | 0.3548 mL | 0.8869 mL | |
| 80 mM | 0.0266 mL | 0.1330 mL | 0.2661 mL | 0.6652 mL | |
| 100 mM | 0.0213 mL | 0.1064 mL | 0.2129 mL | 0.5322 mL |
Ulixertinib hydrochloride Related Classifications
HY-15816A Related Classifications
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