Cat.NO.:A184967 Purity:98+%
Product Details of BMS-754807
| CAS No. : | 1001350-96-4 |
| Formula : |
C23H24FN9O |
| M.W : |
461.49
|
| SMILES Code : | O=C([C@@]1(C)N(C(N=C2NC3=NNC(C4CC4)=C3)=NN5C2=CC=C5)CCC1)NC6=CC=C(F)N=C6 |
| MDL No. : | MFCD18633202 |
| InChI Key : | LQVXSNNAFNGRAH-QHCPKHFHSA-N |
| Pubchem ID : | 24785538 |
Safety of BMS-754807
| GHS Pictogram: |  |
| Signal Word: | Warning |
| Hazard Statements: | H302-H315-H319-H335 |
| Precautionary Statements: | P261-P305+P351+P338 |
Related Pathways of BMS-754807
- RTK
- MAPK
Isoform Comparison
Biological Activity
| Target |
|
In Vitro:
| Concentration | Treated Time | Description | References |
| HCT116 cells | 240 nM | 48-72 hours | BMS-754807 treatment significantly induced p70S6K1 phosphorylation, indicating that IGF-1R inhibition activates p70S6K1 via MEK1/2 to promote cell survival | PMC7447751 |
| SW480 cells | 240 nM | 48-72 hours | BMS-754807 treatment significantly induced p70S6K1 phosphorylation, indicating that IGF-1R inhibition activates p70S6K1 via MEK1/2 to promote cell survival | PMC7447751 |
| MCF-7/AC-1 cells | 10 μmol/L | 24 hours | To evaluate the effect of BMS-754807 alone or in combination with hormonal therapies on the proliferation of MCF-7/AC-1 cells, results showed that BMS-754807 combined with 4-hydroxytamoxifen, letrozole, or fulvestrant had significant antiproliferative effects. | PMC4004036 |
| HCT116 cells | 240 nM | 48 and 72 hours | Induced p70S6K1 phosphorylation, indicating activation of p70S6K1 through inhibition of IGF-1R signaling pathway | PMC7447751 |
| SW480 cells | 240 nM | 48 and 72 hours | Induced p70S6K1 phosphorylation, indicating that this induction is independent of K-Ras or PIK3CA mutations | PMC7447751 |
| HT29-P cells | 240 nM | 24 to 72 hours | Induced p70S6K1 phosphorylation, indicating that Pdcd4 knockdown enhanced BMS-754807-induced activation of p70S6K1, promoting cell survival | PMC7447751 |
| HCT116 cells | 240 nM | 72 hours | Inhibition of p70S6K1 activation led to cell death, indicating that p70S6K1 phosphorylation is a key event for cell survival | PMC7447751 |
| Pa01C | 200 nM | 72 hours | To evaluate the effect of BMS-754807 combined with CQ on PDAC cell proliferation, the results showed that the combination significantly increased cytotoxicity. | PMC8886214 |
| Pa14C | 200 nM | 72 hours | To evaluate the effect of BMS-754807 combined with CQ on PDAC cell proliferation, the results showed that the combination significantly increased cytotoxicity. | PMC8886214 |
| mT4 | 200 nM | 72 hours | To evaluate the effect of BMS-754807 combined with CQ on PDAC cell proliferation, the results showed that the combination significantly increased cytotoxicity. | PMC8886214 |
| breast cancer cell lines | 0.1 μM to 25 μM | 72 hours | To test the sensitivity of BMS-754807 in various breast cancer cell lines, results showed that triple-negative breast cancer cell lines were most sensitive to BMS-754807 | PMC3073089 |
| MIA-PaCa-2 cells | 125 nM | 72 hours | The combination of BMS-754807 and PD-0332991 significantly inhibited the proliferation of MIA-PaCa-2 cells, showing a synergistic effect. | PMC4122288 |
| PSN1 cells | 2.5-10 nM | 2 hours and 16 hours | The combination of BMS-754807 and PD-0332991 significantly inhibited the phosphorylation of S6K1 in PSN1 cells, showing a synergistic effect. | PMC4122288 |
| SMS-CTR | 0 to 1000 nM | 48 hours | To assess the impact of trametinib and ganitumab on apoptosis, results showed that trametinib alone or in combination with ganitumab increased the apoptosis rate in SMS-CTR cells. | PMC9852065 |
| RD | 0 to 1000 nM | 48 hours | To assess the impact of trametinib and ganitumab on apoptosis, results showed that trametinib alone or in combination with ganitumab increased the apoptosis rate in RD cells. | PMC9852065 |
In Vivo:
| Administration | Dosage | Frequency | Description | References |
| Nude mice | HCT116 cell xenograft model | Intraperitoneal injection | 100 mg/kg | Once daily for 3 weeks | The combination of BMS-754807 and U0126 significantly suppressed tumor growth, indicating that inhibition of MEK1/2 overcomes IGF-1R inhibition-induced p70S6K1 activation to promote cell death | PMC7447751 |
| nude mice | MCF-7/AC-1 xenograft model | oral | 75 mg/kg | Twice daily, continued until the end of the experiment | To evaluate the antitumor activity of BMS-754807 alone or in combination with tamoxifen or letrozole in MCF-7/AC-1 xenografts, results showed that combination therapy significantly enhanced tumor regression without major side effects. | PMC4004036 |
| Nude mice | HCT116 cell-derived tumor xenograft model | Intraperitoneal injection | 50 mg/kg/d | once daily for 28 days | Combination of BMS-754807 and U0126 significantly suppressed tumor growth, indicating that inhibition of MEK1/2 abolishes BMS-754807-induced p70S6K1 phosphorylation and promotes cell death | PMC7447751 |
| C57Bl/6 mice | mT4 cell xenograft model | Subcutaneous injection | 25 mg/kg | Once daily for 12 days | To evaluate the effect of BMS-754807 combined with HCQ on tumor growth in the mT4 cell xenograft model, the results showed that the combination significantly reduced tumor burden. | PMC8886214 |
| mice | triple-negative breast cancer tumorgraft model | oral | 10 mg/kg | Once daily for 11 consecutive days | To test the efficacy of BMS-754807 alone or in combination with chemotherapy in a triple-negative breast cancer tumorgraft model, results showed that BMS-754807 significantly inhibited tumor growth, and combination with chemotherapy led to complete tumor regression | PMC3073089 |
| Mice | YAPC cell xenograft model | Oral administration | 12.5 mg/kg | Daily until tumors reached 15 mm | The combination of BMS-754807 and PD-0332991 significantly inhibited tumor growth in the YAPC cell xenograft model, showing a synergistic effect. | PMC4122288 |
| SCID beige mice | RAS-mutated RMS xenograft models | oral gavage and intraperitoneal injection | 50mg/kg | once daily for 14 days | To evaluate the tumor growth inhibitory effect of trametinib and ganitumab combination therapy, results showed that the combination significantly inhibited tumor growth and prolonged survival in the SMS-CTR model. | PMC9852065 |
| Mice | Whole-body 12-Gy γ-irradiation injury model | Oral | BMS-754807 15 mg/kg, PD-0332991 75 mg/kg | Every other day for 21 days | To investigate the role of IGF-1 signaling inhibition in intestinal regeneration after radiation injury. Results showed that BMS-754807-treated mice exhibited more pronounced post-irradiation weight loss and impaired intestinal regeneration, characterized by blunted villi, reduced proliferation, and a 20% decrease in regenerating crypts. | PMC7502577 |
Clinical Trial:
| NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
| NCT00898716 | Neoplasms | PHASE1 | COMPLETED | 2025-07-11 | Local Institution, Chuo-Ku, To… More >>kyo, 104-0045, Japan Less << |
| NCT00569036 | Neoplasms|Solid Tumors|Metasta… More >>ses Less << | PHASE1 | COMPLETED | 2025-04-13 | Local Institution, East Melbou… More >>rne, Victoria, 3002, Australia|Local Institution, Footscray, Victoria, 3011, Australia|Local Institution, Heidelberg, Victoria, 3084, Australia|Local Institution, Parkville, Victoria, 3050, Australia|Local Institution, Nedlands, Western Australia, 6009, Australia Less << |
Protocol
| Bio Calculators | ||||
| Preparing Stock Solutions |  |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.83mL 2.17mL 1.08mL |
21.67mL 4.33mL 2.17mL |
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| Dissolving Methods |
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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