Search Site
Related Products
R428Selective Axl inhibitor

R428

Catalog No. A8329
Size Price Stock Qty
10mM (in 1mL DMSO) $350.00 In stock
1mg $150.00 In stock
5mg $336.00 In stock
10mg $528.00 In stock
50mg $1,600.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Tabata T, Petitt M, et al. "Zika Virus Targets Different Primary Human Placental Cells, Suggesting Two Routes for Vertical Transmission. Cell Host Microbe." 2016 Aug 10;20(2):155-66. PMID:27443522

Quality Control

Chemical structure

R428

Related Biological Data

R428

Related Biological Data

R428

Biological Activity

Description R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl.
Targets Axl          
IC50 14 nM          

Protocol

Cell experiment:[1]

Cell lines

MDA-MB-231 cells, 4T1 cells and Hela cells.

Preparation method

TThe solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

Five-point R428 dose titration (≤ 10 μM); Cells were preincubated with R428 for 3 h.

Applications

R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.

Animal experiment:[2]

Animal models

Female BALB/c mice were inoculated in the mammary fat pad with 0.5 × 106 4T1 cells.

Dosage form

Oral dosing with R428 (7–75 mg/kg twice daily) or vehicle continued until days 19 to 21.

Applications

Oral administration of R428 displayed a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. R428 administration reduced metastatic burden and extended survival in MDAMB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Holland SJ, Pan A, Franci C et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54.

R428 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

R428 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 1037624-75-1 SDF Download SDF
Synonyms R-428;R 428;BGB324
Chemical Name 1-(6,7-dihydro-5H-benzo[2,3]cyclohepta[2,4-d]pyridazin-3-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine
Canonical SMILES C1CCN(C1)C2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76
Formula C30H34N8 M.Wt 506.64
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Background

R428 is a selective Axl inhibitor with an IC50 of 14 nM, more than 50-fold sensitivity for Axl than Abl, Mer, Tyro3, InsR, EGFR, HER2, and PDGFR.

Axl receptor tyrosine kinase transduces signals from extracellular matrix into cytoplasma by binding to the vitamin K-dependent protein growth arrest-specific 6 (Gas6). It is involved in several cellular processes including growth, migration, aggregation and anti-inflammation.

R428 blocks the catalytic activity of Axl, at low nanomolar concentration. [1] Axl-dependent activities, including Akt phosphorylation, cell invasion, proinflammatory cytokine production are inhibited. R428 administration reduces the expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. It also inhibits angiogenesis, reduces metastatic tumor burden and extends survival in animal xenograft models. In addition, R428 synergizes with cisplatin to enhance suppression of liver micrometastasis.

R428 can be administrated orally.

References:
[1]Holland SJ, Pan A, Franci C, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolong survival in models of metastatic breast cancer. Cancer Res 2010. 70(4): 1544-1554.