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Chemical Structure| 1140909-48-3 Chemical Structure| 1140909-48-3

Structure of Cabozantinib S-malate
CAS No.: 1140909-48-3

Chemical Structure| 1140909-48-3

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Cabozantinib S-malate (XL184 S-malate) is a potent inhibitor of multiple receptor tyrosine kinases, including VEGFR2, c-Met, Kit, Axl, and Flt3, with IC50 values of 0.035, 1.3, 4.6, 7, and 11.3 nM, respectively.

Synonyms: XL184 S-malate; BMS-907351 S-malate; XL184

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Product Details of Cabozantinib S-malate

CAS No. :1140909-48-3
Formula : C32H30FN3O10
M.W : 635.59
SMILES Code : O=C(O)[C@@H](O)CC(O)=O.O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C=C3
Synonyms :
XL184 S-malate; BMS-907351 S-malate; XL184
MDL No. :MFCD20923480
InChI Key :HFCFMRYTXDINDK-WNQIDUERSA-N
Pubchem ID :25102846

Safety of Cabozantinib S-malate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Cabozantinib S-malate

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR2

    VEGFR2/KDR, IC50:0.035 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HLE IC50 24 h Inhibited cell cycle progression, reduced proliferation, and induced apoptosis PMC8089119
MHCC97-H IC50 24 h Inhibited cell cycle progression, reduced proliferation, and induced apoptosis PMC8089119
ACHN 1–30 μM 24 h To evaluate the effect of Cabozantinib on the viability of renal cancer cells, showing a dose-dependent decrease in cell viability. PMC10628632
786-0 1–30 μM 24 h To evaluate the effect of Cabozantinib on the viability of renal cancer cells, showing a dose-dependent decrease in cell viability. PMC10628632
HepG2NTCP cells 100 nM 7 days Cabozantinib inhibits HBV RNA transcription by decreasing the binding of phosphorylated STAT3 to the enhancer region 1 of cccDNA through the HGF-MET-STAT3 signaling axis. PMC10635605
RAW264.7 pre-osteoclasts 100 nM and 500 nM 5 days Cabozantinib inhibited RANKL-induced differentiation of RAW264.7 cells into osteoclasts, reducing TRAP activity by 26% and 50%, respectively. PMC7272308
MC3T3-E1 pre-osteoblasts 100 nM 6 days Cabozantinib enhanced osteoblast differentiation, as demonstrated by increases in mRNA and protein levels of ALP and OSC, as well as in calcium deposits. PMC7272308

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice C-Met/β-catenin, Akt/c-Met, Akt/Ras, c-Myc HCC models Oral 60 mg/kg Once daily for 3 weeks In c-Met/β-catenin and Akt/c-Met models, Cabozantinib treatment led to stable disease, but it was ineffective in Akt/Ras and c-Myc models PMC8089119
Nude mice Renal cancer xenograft model Intraperitoneal injection 15 mg/kg Every alternate day for three weeks To evaluate the effect of Cabozantinib and Honokiol combination therapy on tumor growth in a renal cancer xenograft model, showing significant inhibition of tumor growth. PMC10628632
Mice Liver cancer model Oral 30 mg/kg Daily until the end of the study Cabozantinib alone significantly increased neutrophil infiltration and reduced intra-tumour CD8+PD1+T cell proportions, while the combination with anti-PD1 further stimulated both effects and significantly decreased Treg infiltration. PMC9167725
SCID mice Bo-786 RCC bone metastasis model Oral gavage 20 mg/kg Twice daily, 6 days a week for 18 to 39 days Cabozantinib inhibited the growth of Bo-786 RCC in bone, reduced bone osteolysis, increased bone volume and osteoblast number, and decreased osteoclast number and blood vessel density. PMC7272308
C57BL/6J mice HCC mouse model Oral 30 mg/kg Daily until the end of the study The combination of cabozantinib and anti-PD1 showed increased anti-tumour efficacy compared to monotherapy and placebo, significantly increasing neutrophil infiltration and reducing intra-tumour CD8+PD1+T cell proportions, while significantly decreasing Treg infiltration. PMC9167725

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.87mL

1.57mL

0.79mL

15.73mL

3.15mL

1.57mL

References

 

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