Ravoxertinib (GDC-0994)

Catalog No.S7554 Batch:S755407

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Technical Data

Formula

C21H18ClFN6O2
Molecular Weight 439.85 CAS No. 1453848-26-4
Solubility (25°C)* In vitro DMSO 87 mg/mL (197.79 mM)
Ethanol 87 mg/mL (197.79 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
Targets
ERK2 [1]
(Cell-free assay)		 ERK1 [1]
(Cell-free assay)
0.3 nM 1.1 nM
In vitro

GDC-0994 potently inhibits phospho-p90RSK in tumor cells. [1]
In vivo

GDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. [1]

In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival. [2]

Protocol (from reference)

Animal Study:

[4]
  • Animal Models

    Mice

  • Dosages

    40 µg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Blood, 2018, 131(18):2047-2059]

Data from [Data independently produced by , , Biochim Biophys Acta, 2015, 1852(12):2671-7]

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2017, 486(4):1062-1068]

Data from [Data independently produced by , , Cell Immunol, 2017, 314:63-72]

Selleck's Ravoxertinib (GDC-0994) has been cited by 67 publications

DUSP22 Ameliorates Endothelial-to-Mesenchymal Transition in HUVECs through Smad2/3 and MAPK Signaling Pathways [ Cardiovasc Ther, 2024, 2024:5583961] PubMed: 38495810
Transcriptional and chromatin profiling of human blood innate lymphoid cell subsets sheds light on HIV-1 pathogenesis [ EMBO J, 2023, e114153.] PubMed: 37382276
Tetrandrine synergizes with MAPK inhibitors in treating KRAS-mutant pancreatic ductal adenocarcinoma via collaboratively modulating the TRAIL-death receptor axis [ Pharmacol Res, 2023, 197:106955] PubMed: 37820855
High-Throughput Functional Evaluation of MAP2K1 Variants in Cancer [ Mol Cancer Ther, 2023, 22(2):227-239] PubMed: 36442478
ERK1/2-Dependent Phosphorylation of GABAB1(S867/T872), Controlled by CaMKIIβ, Is Required for GABAB Receptor Degradation under Physiological and Pathological Conditions [ Int J Mol Sci, 2023, 24(17)13436] PubMed: 37686242
ERK1/2-Dependent Phosphorylation of GABAB1-S867/T872), Controlled by CaMKIIβ, Is Required for GABAB Receptor Degradation under Physiological and Pathological Conditions [ Int J Mol Sci, 2023, 24(17)13436] PubMed: 37686242
Urinary Eubacterium sp. CAG:581 Promotes Non-Muscle Invasive Bladder Cancer (NMIBC) Development through the ECM1/MMP9 Pathway [ Cancers (Basel), 2023, 15(3)809] PubMed: 36765767
Urinary Eubacterium sp. CAG:581 Promotes Non-Muscle Invasive Bladder Cancer (NMIBC) Development through the ECM1/MMP9 Pathway [ Cancers (Basel), 2023, 15(3)809] PubMed: 36765767
A Chemical Proteomics Approach to Discover Regulators of Innate Immune Signaling [ Viruses, 2023, 15(5)1112] PubMed: 37243198
Synergism of Carbamoylated Erythropoietin and Insulin-like Growth Factor-1 in Immediate Early Gene Expression [ Life (Basel), 2023, 13(9)1826] PubMed: 37763230

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.