Ravoxertinib benzenesulfonate
Based on 48 publication(s) in Google Scholar
Ravoxertinib benzenesulfonate (GDC-0994 benzenesulfonate) is an orally active ERK1/2 inhibitor. Ravoxertinib benzenesulfonate inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib benzenesulfonate decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib benzenesulfonate can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 1817728-45-2
- Formula: C27H24ClFN6O5S
- Molecular Weight:599.03
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Ravoxertinib benzenesulfonate
More- Nature. 2025 Jan;637(8046):726-735. [Abstract]
- Cancer Cell. 2023 Jul 10;41(7):1345-1362.e9. [Abstract]
- Cell. 2018 Sep 20;175(1):186-199.e19. [Abstract]
- Nat Metab. 2022 Mar;4(3):374-388. [Abstract]
- Nat Aging. 2026 Jul;6(7):1395-1416.
- Cell Mol Immunol. 2023 Feb;20(2):175-188. [Abstract]
- Nat Commun. 2026 Jan 21;17(1):1902. [Abstract]
- Nat Commun. 2023 Sep 30;14(1):6117. [Abstract]
- Cell Discov. 2026 Feb 24;12(1):13. [Abstract]
- Redox Biol. 2023 Sep:65:102825. [Abstract]
- Sci Transl Med. 2021 Jan 27;13(578):eaba7308. [Abstract]
- J Exp Clin Cancer Res. 2023 Jul 13;42(1):166. [Abstract]
- Cell Rep Med. 2025 Feb 18;6(2):101970. [Abstract]
- Cell Death Dis. 2021 Dec 1;12(12):1123. [Abstract]
- Diabetes. 2021 Sep;70(9):2131-2146. [Abstract]
- Oncogene. 2021 Jul;40(30):4884-4893. [Abstract]
- Neural Regen Res. 2023 Aug;18(8):1743-1749. [Abstract]
- Clin Transl Med. 2023 Aug;13(8):e1381. [Abstract]
- Stem Cell Res Ther. 2025 Jul 1;16(1):337. [Abstract]
- Cell Rep. 2023 Sep 1;42(9):113048. [Abstract]
- Environ Pollut. 2021 Jan 1;268(Pt B):115748. [Abstract]
- Biochem Pharmacol. 2025 Sep:239:117032. [Abstract]
- Gastric Cancer. 2023 May;26(3):379-392. [Abstract]
- Int Immunopharmacol. 2025 Nov 8;168(Pt 1):115798. [Abstract]
- Zool Res. 2022 Jul 18;43(4):537-551. [Abstract]
- Cancer. 2020 Mar 15;126(6):1339-1350. [Abstract]
- Cancers (Basel). 2022 May 19;14(10):2493. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- Cell Signal. 2023 May:105:110607. [Abstract]
- J Cell Mol Med. 2020 Sep;24(17):10151-10165. [Abstract]
- iScience. 2024 Sep 12;27(10):110873. [Abstract]
- Mol Oncol. 2020 Nov;14(11):2894-2919. [Abstract]
- J Pharmacol Exp Ther. 2020 Jul;374(1):104-112. [Abstract]
- Proteomics. 2023 Aug;23(16):e2300041. [Abstract]
- Exp Mol Pathol. 2021 Feb:118:104587. [Abstract]
- Am J Physiol Heart Circ Physiol. 2018 Mar 1;314(3):H580-H592. [Abstract]
- Int J Med Sci. 2022 Jan 1;19(1):195-204. [Abstract]
- Biochem Biophys Rep. 2026 Jan 15:45:102454. [Abstract]
- Am J Cancer Res. 2020 Nov 1;10(11):3622-3643. [Abstract]
- J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
- Reprod Sci. 2020 Feb;27(2):704-712. [Abstract]
- Toxicol In Vitro. 2020 Jun:65:104777. [Abstract]
- Biochem Biophys Res Commun. 2021 May 21:554:63-70. [Abstract]
- Université de Lausanne. 2024 Feb 7.
- Indian J Pharm Sci. 2022.
- Universität Würzburg. 2021 Jan.
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
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Cell Proliferation/Viability Assay
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RT-PCR
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RT-PCR
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IP
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RT-PCR
Biological Activity
Description
IC50 & Target
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ERK2 3.1 nM (IC50) |
ERK1 6.1 nM (IC50) |
p-RSK 12 nM (IC50) |
In Vitro
In relevant in vitro experiments on stem cell-like human glioma stem cells, Ravoxertinib benzenesulfonate completely abrogates Humanin (HY-P1928)-induced Temozolomide (HY-17364) resistance, restores the growth inhibitory effect of Temozolomide on tumor cells, and inhibits the Humanin-induced upregulation of Hus1 protein expression[1].
Combination of Ravoxertinib (0.1-10 μM; 7 d) benzenesulfonate and ipatasertib induces additive to superadditive cytotoxicity in multiple human tumor organoid spheres, with over 2-log cell killing achieved in the 417821-307-R-J1 lung squamous cell carcinoma organoid spheres[2].
Ravoxertinib (1 μM; 72 h) benzenesulfonate does not significantly inhibit the LMCD1-mediated enhancement of cell proliferation in human dermal fibroblasts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ravoxertinib (20-30 mg/kg; p.o.) benzenesulfonate is well tolerated at 20 mg/kg and 30 mg/kg in NSG mice bearing 845751-090-R-J2 head and neck squamous cell carcinoma PDX, but its combination with ipatasertib does not control tumor growth, leading to progressive disease[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1817728-45-2
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Molecular Weight 599.03
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Formula C27H24ClFN6O5S
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SMILES
O=S(O)(C1=CC=CC=C1)=O.OC[C@H](C2=CC(F)=C(C=C2)Cl)N3C(C=C(C4=NC(NC5=CC=NN5C)=NC=C4)C=C3)=O
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Synonyms
GDC-0994 benzenesulfonate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (48)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jan;637(8046):726-735. PMID: 39537929
Ravoxertinib benzenesulfonate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Jan;637(8046):726-735. [Abstract]
Investigation of the signalling axis regulating LIF expression upon PDGF stimulation. Cells were treated with ERK inhibitor ravoxertinib (10 μM) for 24 h before cell lysis for total RNA extraction and measurement of LIF mRNA levels by real-time qPCR.
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Cancer Cell
Antiandrogen treatment induces stromal cell reprogramming to promote castration resistance in prostate cancer. [Abstract]2023 Jul 10;41(7):1345-1362.e9. PMID: 37352863 -
Cell
2018 Sep 20;175(1):186-199.e19. PMID: 30220457 -
Nat Metab
MAPK signalling-induced phosphorylation and subcellular translocation of PDHE1α promotes tumour immune evasion. [Abstract]2022 Mar;4(3):374-388. PMID: 35315437 -
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Cell Mol Immunol
β-adrenoreceptor-triggered PKA activation negatively regulates the innate antiviral response. [Abstract]2023 Feb;20(2):175-188. PMID: 36600052
Ravoxertinib benzenesulfonate purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Feb;20(2):175-188. [Abstract]
Effects of kinase inhibitors on ISO-triggered inhibition of SeV-induced transcription of the IFNB1 gene. THP1 cells were treated with the ERK inhibitor GDC-0994 (1 μM) for 1 h and then were treated with ISO (10 μM) and infected with SeV (MOI = 1). Six hours later, a qPCR analysis to determine the mRNA levels of the IFNB1 gene was performed. The results are shown as the inhibition rate (%).
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Nat Commun
An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]2026 Jan 21;17(1):1902. PMID: 41565660
Ravoxertinib benzenesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Jan 21;17(1):1902. [Abstract]
U87, U251, and H1299 cells, with or without EGFR R252C mutation were treated with or without 5 μM Ravoxertinib. Cell proliferation was assessed at day 7. Relative proliferation was calculated using vehicle-treated EGFR WT cells as the control.
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Nat Commun
IGF1R-phosphorylated PYCR1 facilitates ELK4 transcriptional activity and sustains tumor growth under hypoxia. [Abstract]2023 Sep 30;14(1):6117. PMID: 37777542
Ravoxertinib benzenesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 30;14(1):6117. [Abstract]
HCT116 cells were pretreated with PPP (1 μM), ARQ-092 (2 μM) and GDC-0994 (Ravoxertinib, 10 μM) for 1 h before being cultured under hypoxia for 12 h.
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Cell Discov
ASCT2 palmitoylation regulated by JNK1-ZDHHC14 axis orchestrates glutamine metabolism and NSCLC progression. [Abstract]2026 Feb 24;12(1):13. PMID: 41730846 -
Redox Biol
2023 Sep:65:102825. PMID: 37531930 -
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 -
J Exp Clin Cancer Res
Pulmonary interleukin 1 beta/serum amyloid A3 axis promotes lung metastasis of hepatocellular carcinoma by facilitating the pre-metastatic niche formation. [Abstract]2023 Jul 13;42(1):166. PMID: 37443052
Ravoxertinib benzenesulfonate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Jul 13;42(1):166. [Abstract]
The effect of NF-κB, ERK, JNK and p38 inhibitors on IL-1β-induced Saa3 expression in vivo. One hour after intravenous administration of Ravoxertinib, IL-1β (20 ng in 100 ul saline) were i.v. administrated into the mice. Six hours later, lung Saa3 expression was detected by qPCR.
Ravoxertinib benzenesulfonate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2023 Jul 13;42(1):166. [Abstract]
The effect of NF-κB, ERK, JNK and p38 inhibitors on IL-1β-induced Saa3 expression in MLE-12 cells. MLE-12 cells were pre-treated with Ravoxertinib for 1 h, then stimulated with IL-1β (10 ng/ml) for 6 h. Saa3 expression was detected by qPCR.
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Cell Rep Med
2025 Feb 18;6(2):101970. PMID: 39938523 -
Cell Death Dis
Targeting SYK of monocyte-derived macrophages regulates liver fibrosis via crosstalking with Erk/Hif1α and remodeling liver inflammatory environment. [Abstract]2021 Dec 1;12(12):1123. PMID: 34853322 -
Diabetes
Cardiac Tissue Factor Regulates Inflammation, Hypertrophy, and Heart Failure in Mouse Model of Type 1 Diabetes. [Abstract]2021 Sep;70(9):2131-2146. PMID: 34155039 -
Oncogene
2021 Jul;40(30):4884-4893. PMID: 34163029 -
Neural Regen Res
Overexpression of mitogen-activated protein kinase phosphatase-1 in endothelial cells reduces blood-brain barrier injury in a mouse model of ischemic stroke. [Abstract]2023 Aug;18(8):1743-1749. PMID: 36751800 -
Clin Transl Med
Regulatory roles of Osteopontin in lung epithelial inflammation and epithelial-telocyte interaction. [Abstract]2023 Aug;13(8):e1381. PMID: 37605313 -
Stem Cell Res Ther
Interleukin-1 receptor antagonist overexpression in mesenchymal stem cells improves hemorrhagic cystitis outcomes via HtrA serine peptidase 3. [Abstract]2025 Jul 1;16(1):337. PMID: 40598340 -
Cell Rep
2023 Sep 1;42(9):113048. PMID: 37659078 -
Environ Pollut
BPA modulates the WDR5/TET2 complex to regulate ERβ expression in eutopic endometrium and drives the development of endometriosis. [Abstract]2021 Jan 1;268(Pt B):115748. PMID: 33022573 -
Biochem Pharmacol
Molecular Dissection of the AHR-AREG driven EGFR-ERK1/2-CyclinD1 axis in acquired lenvatinib resistance of Hepatocellular carcinoma. [Abstract]2025 Sep:239:117032. PMID: 40482839 -
Gastric Cancer
2023 May;26(3):379-392. PMID: 36811690 -
Int Immunopharmacol
TMEM176A drives anti-apoptotic signaling through TGM2-mediated ERK activation in gastric cancer. [Abstract]2025 Nov 8;168(Pt 1):115798. PMID: 41207103 -
Zool Res
Production of functional sperm from in vitro-cultured premeiotic spermatogonia in a marine fish. [Abstract]2022 Jul 18;43(4):537-551. PMID: 35616259 -
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 -
Cancers (Basel)
RON ( MST1R) and HGFL ( MST1) Co-Overexpression Supports Breast Tumorigenesis through Autocrine and Paracrine Cellular Crosstalk. [Abstract]2022 May 19;14(10):2493. PMID: 35626096 -
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 -
Cell Signal
2023 May:105:110607. PMID: 36690134 -
J Cell Mol Med
CXXC finger protein 4 inhibits the CDK18-ERK1/2 axis to suppress the immune escape of gastric cancer cells with involvement of ELK1/MIR100HG pathway. [Abstract]2020 Sep;24(17):10151-10165. PMID: 32715641 -
iScience
2024 Sep 12;27(10):110873. PMID: 39398235 -
Mol Oncol
Optimized low-dose combinatorial drug treatment boosts selectivity and efficacy of colorectal carcinoma treatment. [Abstract]2020 Nov;14(11):2894-2919. PMID: 33021054 -
J Pharmacol Exp Ther
2020 Jul;374(1):104-112. PMID: 32434944 -
Proteomics
A proteomic signature and potential pharmacological opportunities in the adaptive resistance to MEK and PI3K kinase inhibition in pancreatic cancer cells. [Abstract]2023 Aug;23(16):e2300041. PMID: 37140101 -
Exp Mol Pathol
Up-regulation of miRNA-151-3p enhanced the neuroprotective effect of dexmedetomidine against β-amyloid by targeting DAPK-1 and TP53. [Abstract]2021 Feb:118:104587. PMID: 33275947 -
Am J Physiol Heart Circ Physiol
Overexpression of the neuronal human (pro)renin receptor mediates angiotensin II-independent blood pressure regulation in the central nervous system. [Abstract]2018 Mar 1;314(3):H580-H592. PMID: 29350998 -
Int J Med Sci
The Fgl2 interaction with Tyrobp promotes the proliferation of cutaneous squamous cell carcinoma by regulating ERK-dependent autophagy. [Abstract]2022 Jan 1;19(1):195-204. PMID: 34975313 -
Biochem Biophys Rep
2026 Jan 15:45:102454. PMID: 41584303 -
Am J Cancer Res
ERRα promotes pancreatic cancer progression by enhancing the transcription of PAI1 and activating the MEK/ERK pathway. [Abstract]2020 Nov 1;10(11):3622-3643. PMID: 33294258 -
J Cell Biochem
Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]2020 Mar;121(3):2343-2353. PMID: 31633245 -
Reprod Sci
Bisphenol A Exposure Enhances Endometrial Stromal Cell Invasion and Has a Positive Association with Peritoneal Endometriosis. [Abstract]2020 Feb;27(2):704-712. PMID: 32046440 -
Toxicol In Vitro
Combined SRPK and AKT pharmacological inhibition is synergistic in T-cell acute lymphoblastic leukemia cells. [Abstract]2020 Jun:65:104777. PMID: 31962201 -
Biochem Biophys Res Commun
MAL2 interacts with IQGAP1 to promote pancreatic cancer progression by increasing ERK1/2 phosphorylation. [Abstract]2021 May 21:554:63-70. PMID: 33780861 -
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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 -
Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Purity & Documentation
References
[2]. Teicher BA, et al. Targeted therapy combinations with ipatasertib in multi-cell type 3D tumor spheroid models. Acad Oncol. 2025;2(2):10.20935/acadonco7726. [Content Brief]
[3]. Ye Z, et al. LMCD1 facilitates the induction of pluripotency via cell proliferation, metabolism, and epithelial-mesenchymal transition. Cell Biol Int. 2022;46(9):1409-1422. [Content Brief]
[4]. Hunt BG, et al. RON-augmented cholesterol biosynthesis in breast cancer metastatic progression and recurrence. Oncogene. 2023;42(21):1716-1727. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)