R428

CAS No.
1037624-75-1
Chemical Name:
R428
Synonyms
R428;CS-1130;BGB-324;EOS-62006;Bemcentinib;R428 (BGB324);BGB324 (R428);R428 USP/EP/BP;BGB-324, CPDB1725;Bemcentinib Crude
CBNumber:
CB42621146
Molecular Formula:
C30H34N8
Molecular Weight:
506.64
MDL Number:
MFCD21608463
MOL File:
1037624-75-1.mol
Last updated:2023-09-26 20:09:08

R428 Properties

Melting point >211°C (dec.)
Boiling point 799.6±70.0 °C(Predicted)
Density 1.41±0.1 g/cm3(Predicted)
storage temp. -20°C
solubility Soluble in DMSO (up to at least 25 mg/ml)
pka 10.34±0.20(Predicted)
form Yellow powder.
color Yellow
Stability Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
FDA UNII 0ICW2LX8AS

SAFETY

Risk and Safety Statements

NFPA 704
0
2 0

R428 price More Price(30)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21523 R428 ≥98% 1037624-75-1 1mg $68 2024-03-01 Buy
Cayman Chemical 21523 R428 ≥98% 1037624-75-1 10mg $601 2024-03-01 Buy
Cayman Chemical 21523 R428 ≥98% 1037624-75-1 25mg $1002 2024-03-01 Buy
TRC R060020 R428 1037624-75-1 1mg $50 2021-12-16 Buy
ApexBio Technology A8329 R428 1037624-75-1 1mg $65 2021-12-16 Buy
Product number Packaging Price Buy
21523 1mg $68 Buy
21523 10mg $601 Buy
21523 25mg $1002 Buy
R060020 1mg $50 Buy
A8329 1mg $65 Buy

R428 Chemical Properties,Uses,Production

Description

R428 (bemcentinib, BGB324), a selective small-molecule inhibitor of AXL, is currently being evaluated in phase II trials for the treatment of non-small-cell lung cancer (NSCLC) and acute myelocytic leukemia (AML). It has been found to induce apoptosis in cancer cells and to block tumor spread in models of metastatic breast cancer. The therapeutic potential of R428 has also been demonstrated in highly invasive esophageal adenocarcinoma cells and in ESCC cells.
R428 is a selective, small molecule inhibitor of Axl that blocks its catalytic and precancerous activities. R428 treatment reduced Axl-induced AKT phosphorylation, cancer cell invasion, angiogenesis, and the production of pro-inflammatory cytokines. It also reduced the expression of the cytokine granulocyte macrophage colony-stimulating factor and Snail in a dosage-dependent manner. Interestingly,using R428 to inhibit Axl-mediated cellular and molecular functions during cisplatin treatments achieved an enhanced suppression of liver metastases. Axl knockdowns in RAC cell lines reduced migration, invasion, and in vivo engraftment, accompanied by a downregulation in the activity of the Ral GTPase proteins (RalA and RalB). Similar effects were obtained using an A428 inhibitor. Blocking Axl functions also abrogated the phosphorylation of ERBB2 (Her-2/neu) at the Tyr877 residue, which reveals the cross-functional effects of R428 on different receptor signaling axes.
Cabozantinib (XL184) and R428 (BGB324) Inhibit the Growth of Esophageal Squamous Cell Carcinoma (ESCC)

Uses

R 428 is an AXL tyrosine kinase inhibitor shown to be used as an anti-cancer agent.

target

Axl

References

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

R428 Preparation Products And Raw materials

Raw materials

Preparation Products