Bemcentinib (R428)

Catalog No.S2841 Batch:S284112

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Technical Data

Formula

C30H34N8
Molecular Weight 506.64 CAS No. 1037624-75-1
Solubility (25°C)* In vitro DMSO 8 mg/mL (15.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
Targets
Axl [1]
(Cell-free assay)
14 nM
In vitro R428 blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. [1] In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of ∼ 2.0μM for the primary CLL B cells after 24 hours of treatment and normal B-, T-, and natural killer (NK) cells show no significant amount of cell death at this dose of R428 (2.5 μM) under similar experimental conditions. [2]
In vivo Pharmacologic investigations reveal favorable exposure after oral administration such that R428-treated tumors display a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibits angiogenesis in corneal micropocket and tumor models. R428 administration reduces metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. [1]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    MDA-MB-231-luc-D3H2LN Intracardiac Model

  • Dosages

    125 mg/kg

  • Administration

    Oral, twice daily

Customer Product Validation

Data from [Data independently produced by Cancer Res, 2014, 74(18), 5152-64]

Data from [Data independently produced by Biochem Bioph Res Co, 2014, 10.1016/j.bbrc.2014.10.126]

, , FASEB J, 2017, 31(4):1382-1397

Data from [Data independently produced by , , Blood, 2018, doi:10.1182/blood-2018-05-853291]

Selleck's Bemcentinib (R428) has been cited by 122 publications

Impact of sunitinib resistance on clear cell renal cell carcinoma therapeutic sensitivity in vitro [ Cell Cycle, 2024, 1-13.] PubMed: 38263737
MUC1-C Is a Common Driver of Acquired Osimertinib Resistance in NSCLC [ J Thorac Oncol, 2023, 10.1016/j.jtho.2023.10.017] PubMed: 37924972
Single cell analysis in head and neck cancer reveals potential immune evasion mechanisms during early metastasis [ Nat Commun, 2023, 14(1):1680] PubMed: 36973261
Inhibition of AXL receptor tyrosine kinase enhances brown adipose tissue functionality in mice [ Nat Commun, 2023, 14(1):4162] PubMed: 37443109
Extracellular matrix-derived peptide stimulates the generation of endocrine progenitors and islet organoids from iPSCs [ J Tissue Eng, 2023, 14:20417314231185858] PubMed: 37435573
CDK8/19 inhibition plays an important role in pancreatic β-cell induction from human iPSCs [ Stem Cell Res Ther, 2023, 14(1):1] PubMed: 36600289
AXL Expression on Homeostatic Resident Liver Macrophages Is Reduced in Cirrhosis Following GAS6 Production by Hepatic Stellate Cells [ Cell Mol Gastroenterol Hepatol, 2023, 16(1):17-37] PubMed: 37004869
Regulation of brain endothelial cell physiology by the TAM receptor tyrosine kinase Mer [ Commun Biol, 2023, 6(1):916] PubMed: 37673933
Regulation of brain endothelial cell physiology by the TAM receptor tyrosine kinase Mer [ Commun Biol, 2023, 6(1):916] PubMed: 37673933
The effect of inhibition of receptor tyrosine kinase AXL on DNA damage response in ovarian cancer [ Commun Biol, 2023, 6(1):660] PubMed: 37349576

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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.