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Product Details

R428 | Potent and selective AXL inhibitor

R428 (1037624-75-1) is a potent and selective inhibitor of AXL kinase (IC50 = 1.4nM).1 R428 has been shown to overcome chemotherapy resistance to various agents in multiple cancer models.2-5 AXL has been shown to suppress myeloid cell activation and function – combined AXL inhibition with R428 and PD-1 blockade showed potent synergistic antitumor effects.6,7

References/Citations

1) Holland et al. (2010), R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer; Cancer Res. 70 1544
2) Fleuren et al. (2014), The role of AXL and the in vitro activity of the receptor tyrosine kinase inhibitor BGB324 in Ewing sarcoma; Oncotarget 5 12753
3) Xu et al. (2014), Inhibition of Axl improves the targeted therapy against ALK-mutated neuroblastoma; Biochem. Biophys. Res. Commun. 454 566
4) Ben-Batalla et al. (2017), Axl Blockade by BGB324 Inhibits BCR-ABL Tyrosine Kinase Inhibitor-Sensitive and -Resistant Chronic Myeloid Leukemia; Clin. Cancer Res. 23 2289
5) Lin et al. (2017), Targeting AXL overcomes resistance to docetaxel therapy in advanced prostate cancer; Oncotarget 8 41064
6) Guo et al. (2017), Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models; Oncotarget 8 89761
7) Ludwig et al. (2018), Small-Molecule Inhibition of Axl Targets Tumor Immune Suppression and Enhances Chemotherapy in Pancreatic Cancer; Cancer Res. 78 246

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Catalog#  10-4676-0005

$90.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1037624-75-1
Catalog Number:
10-4676
Activity:
Potent and selective AXL inhibitor
Chemical Name:
1-(3,4-Diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-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
Alternate Names:
Bemcentinib; BGB324
Molecular Weight:
506.64
Molecular Formula:
C30H34N8
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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