R428 | Potent and selective AXL inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $275.00 |
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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
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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