Structure of CP-673451
CAS No.: 343787-29-1
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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.
CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits > 450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity.
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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'.
Search for reports by entering the product batch number.
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Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 343787-29-1 |
Formula : | C24H27N5O2 |
M.W : | 417.50 |
SMILES Code : | NC1CCN(C2=C3N=C(N4C=NC5=CC(OCCOC)=CC=C45)C=CC3=CC=C2)CC1 |
MDL No. : | MFCD11100329 |
InChI Key : | DEEOXSOLTLIWMG-UHFFFAOYSA-N |
Pubchem ID : | 10158940 |
GHS Pictogram: |
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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 |
Human placental pericytes | 0.01–100 µM | 24 hours | To measure the direct effects of sunitinib on pericyte viability, showing a dose-dependent impairment of pericyte viability. | PMC3833098 |
Ba/F3 cells | 9.448 nM | 72 hours | To evaluate the inhibitory effect of CP-673451 on the MYH9::PDGFRB fusion gene, results showed that Ba/F3 cells were highly sensitive to CP-673451 | PMC11063843 |
CTV-1 cells | 230 nM | 72 hours | To evaluate the inhibitory effect of CP-673451 on CTV-1 cells, results showed that CTV-1 cells were sensitive to CP-673451 | PMC11063843 |
T-ALL1 PDX cells | <5 nM | 72 hours | To evaluate the inhibitory effect of CP-673451 on T-ALL1 PDX cells, results showed that T-ALL1 PDX cells were highly sensitive to CP-673451 | PMC11063843 |
Pten−/−MEFs | 2 μM | 24 hours | To evaluate the effect of MK-2206 on PDGFRα expression in Pten−/−MEFs. Results showed that MK-2206 significantly inhibited PDGFRα expression. | PMC7876135 |
U373 cells | 5 μM | 24 hours | To evaluate the effect of MK-2206 on PDGFRα expression in U373 cells. Results showed that MK-2206 significantly inhibited PDGFRα expression. | PMC7876135 |
RAW264.7 macrophages | 20 μg/mL | 8, 16, 24 hours | To investigate the effect of CP-673451 on the transcription levels of CCL1, CCL2, CCL7, CXCL11, IL-1β, IL-6, IL-10, and TNF-α in LPS-stimulated RAW264.7 macrophages, results showed that CP-673451 significantly reduced the transcription levels of CCL2, CCL7, IL-10, and TNF-α. | PMC6841710 |
Human brain vascular pericytes | 10 ng/mL | 4 hours | To evaluate the effect of TGF-β on the expression of pSMAD3 and KLF4 in HBVPs, results showed that TGF-β significantly increased the expression of pSMAD3 and KLF4. | PMC9713377 |
U87 GBM cells | 1 μM | 24 hours | triggers outgrowth of neurite-like processes, suggesting differentiation into neural-like cells | PMC9076540 |
G166 GSCs | 1 μM | 48 hours | significantly increased the average neurite-like process length, indicating differentiation | PMC9076540 |
GS090 GSCs | 1 μM | 48 hours | significantly increased the average neurite-like process length, indicating differentiation | PMC9076540 |
G179 GSCs | 1 μM | 48 hours | significantly increased the average neurite-like process length, indicating differentiation | PMC9076540 |
bovine embryonic cells | 100 nM | 3 days | To investigate the inhibitory effect of CP-673451 on PDGFR and its impact on NFYA expression and bovine embryonic development. Results showed that CP-673451 significantly reduced NFYA expression and nuclear localization, and decreased the developmental rate of bovine embryos. | PMC10707662 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Sprague–Dawley (SD) rats | sepsis model | gastric gavage | 100 mg/kg | Single dose | CP-673451 was used to selectively inhibit PDGFR-β. After 7 consecutive days of administration, it successfully reduced the amount of vascular pericytes within the rat mesentery and decreased the expression of pericyte markers (NG-2 and PDGFR-β) in mesenteric microvascular networks. | PMC10010010 |
Mice | Oral gavage | 75 mg/kg/day | Once daily for 14 days | To evaluate the effects of CP-673451 on cardiac function in mice, showing a decrease in ejection fraction and coronary flow reserve, similar to the effect seen with sunitinib. | PMC3833098 | |
NSG-SGM3 mice | T-ALL patient-derived xenograft model | intraperitoneal injection | 10 mg/kg | once daily for 10 weeks | To evaluate the therapeutic effect of CP-673451 on the T-ALL1 PDX model, results showed that CP-673451 significantly delayed leukemia progression | PMC11063843 |
Nude mice | U373 cell subcutaneous xenograft model | Intraperitoneal injection | ceritinib (30 mg/kg), AZD1208 (15 mg/kg) | daily for 14 days | To evaluate the therapeutic efficacy of MK-2206 and CP-673451 alone or in combination on U373 cell subcutaneous xenografts. Results showed that the combination of MK-2206 and CP-673451 significantly inhibited tumor growth. | PMC7876135 |
mice | cecal ligation puncture (CLP) model | gavage | 10 mg/kg | 3 times a week for 2 weeks | To investigate the effect of CP-673451 on the survival rate of CLP model mice, results showed that CP-673451 significantly decreased the mortality of CLP mice. | PMC9345782 |
Mice | Ccm1ECKO mice | Intraperitoneal injection | 200 mg/kg | administered at 2, 24, 48, and 72h after CLP | To evaluate the effect of CP-673451 on pericyte function in Ccm1ECKO mice, results showed that CP-673451 significantly downregulated PDGFRβ expression and exacerbated CCM lesion development. | PMC9713377 |
mice | U87 GBM cell subcutaneous xenograft model | oral | 30 or 60 mg/kg | Every 12 hours for 2 days, repeated weekly for 4 weeks | CP-673451 treatment significantly improved the anti-tumour effects of temozolomide | PMC9076540 |
Sprague-Dawley (SD) rats | Sepsis model | Gastric gavage | 40 mg/(kg·d) | 7 consecutive days | Depletion of pericytes using CP-673451, a selective PDGFR-β inhibitor, to study its role in sepsis. | PMC10010010 |
Tags: CP-673451 | CP673451 | CP 673451 | PDGFR | Platelet-derived growth factor receptor | PDGFR inhibitor | PDGFRα inhibitor | PDGFRβ inhibitor | 343787-29-1
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P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
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H200 | Unstable explosive |
H201 | Explosive; mass explosion hazard |
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H203 | Explosive; fire, blast or projection hazard |
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H221 | Flammable gas |
H222 | Extremely flammable aerosol |
H223 | Flammable aerosol |
H224 | Extremely flammable liquid and vapour |
H225 | Highly flammable liquid and vapour |
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H227 | Combustible liquid |
H228 | Flammable solid |
H229 | Pressurized container: may burst if heated |
H230 | May react explosively even in the absence of air |
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 |
H280 | Contains gas under pressure; may explode if heated |
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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