Ravoxertinib (GDC-0994)

Catalog No.S7554 Batch:S755410

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Technical Data

Formula

C21H18ClFN6O2
Molecular Weight 439.85 CAS No. 1453848-26-4
Solubility (25°C)* In vitro DMSO 88 mg/mL (200.06 mM)
Ethanol 88 mg/mL (200.06 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 73 publications

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] PubMed: 38588697
Targeting ERK-MYD88 interaction leads to ERK dysregulation and immunogenic cancer cell death [ Nat Commun, 2024, 15(1):7037] PubMed: 39147750
Myeloid cells coordinately induce glioma cell-intrinsic and cell-extrinsic pathways for chemoresistance via GP130 signaling [ Cell Rep Med, 2024, S2666-3791(24)00372-0] PubMed: 39053460
Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2 [ Elife, 2024, 12RP91507] PubMed: 38537148
The ERK inhibitor GDC-0994 selectively inhibits growth of BRAF mutant cancer cells [ Transl Oncol, 2024, 45:101991] PubMed: 38728872
HER3 V104 mutations regulate cell signaling, growth, and drug sensitivity in cancer [ Mol Carcinog, 2024, 10.1002/mc.23743] PubMed: 38751013
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

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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.