Structure of Cabozantinib S-malate
CAS No.: 1140909-48-3
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
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 |
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 |
Tags: Cabozantinib | XL184 | BMS-907351 | XL 184 | XL-184 | BMS907351 | BMS 907351 | VEGFR | Apoptosis | Vascular endothelial growth factor receptor | MET inhibitor | VEGFR2 | AXL | RET | multi-targeted kinase inhibitor | c-Met | Flt3 | tyrosine kinase inhibitor | 1140909-48-3
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Response | |
Code | Phrase |
P301 | IF SWALLOWED: |
P304 | IF INHALED: |
P305 | IF IN EYES: |
P306 | IF ON CLOTHING: |
P307 | IF exposed: |
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P378 | |
P380 | Evacuate area. |
P381 | Eliminate all ignition sources if safe to do so. |
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P391 | Collect spillage. Hazardous to the aquatic environment |
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P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
P370 + P378 | In case of fire: |
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P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
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Storage | |
Code | Phrase |
P401 | |
P402 | Store in a dry place. |
P403 | Store in a well-ventilated place. |
P404 | Store in a closed container. |
P405 | Store locked up. |
P406 | Store in corrosive resistant/ container with a resistant inner liner. |
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P413 | |
P420 | Store away from other materials. |
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P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
P411 + P235 | Keep cool. |
Disposal | |
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H201 | Explosive; mass explosion hazard |
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H203 | Explosive; fire, blast or projection hazard |
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H228 | Flammable solid |
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H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
H240 | Heating may cause an explosion |
H241 | Heating may cause a fire or explosion |
H242 | Heating may cause a fire |
H250 | Catches fire spontaneously if exposed to air |
H251 | Self-heating; may catch fire |
H252 | Self-heating in large quantities; may catch fire |
H260 | In contact with water releases flammable gases which may ignite spontaneously |
H261 | In contact with water releases flammable gas |
H270 | May cause or intensify fire; oxidizer |
H271 | May cause fire or explosion; strong oxidizer |
H272 | May intensify fire; oxidizer |
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H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
H290 | May be corrosive to metals |
Health hazards | |
Code | Phrase |
H300 | Fatal if swallowed |
H301 | Toxic if swallowed |
H302 | Harmful if swallowed |
H303 | May be harmful if swallowed |
H304 | May be fatal if swallowed and enters airways |
H305 | May be harmful if swallowed and enters airways |
H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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