BMS-754807 [1001350-96-4]
Référence HY-10200-10mg
Conditionnement : 10mg
Marque : MedChemExpress
BMS-754807 est un inhibiteur de IGF-1R/IR qui est puissant et réversible (IC50=1,8 et 1,7 nM , respectivement; Ki=<2 nM pour les deux). BMS-754807 montre également des activités puissantes contre Met, RON, TrkA, TrkB, AurA et AurB avec des valeurs IC50 de 6, 44, 7, 4, 9 et 25 nM, respectivement.
BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively.
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BMS-754807 Chemical Structure
CAS No. : 1001350-96-4
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Based on 10 publication(s) in Google Scholar
Description |
BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively[1]. |
IC50 & Target |
IC50: 1.7 nM (IR), 1.8 nM (IGF-1R), 4 nM (TrkB), 6 nM (Met), 7 nM (TrkA), 9 nM (AurA), 25 nM (AurB), 44 nM (RON)[1] |
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In Vitro |
BMS-754807 effectively inhibits the growth of a broad range of human tumor cell lines with IC50 values of ranging from 5 to 365 nM. BMS-754807 also inhibits the proliferation of human rhabdomyosarcoma tumor cells Rh41 and human colon carcinoma Geo with IC50s of 7 and 5 nM, respectively. BMS-754807 shows inhibitory activity in the proliferation of Rh41 cells with IC50 of 5 nM[1]. BMS-754807 inhibits the phosphorylation of IGF-1R (IC50=13 nM) and the downstream targets Akt (IC50=22 nM) and MAPK (IC50=13 nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line[2]. BMS-754807 shows a median EC50 value of 0.62 μM against the PPTP cell lines. The median EC50 for the four Ewing sarcoma cell lines is less than that for the remaining PPTP cell lines (0.19 μM vs. 0.78 μM, P=0.0470)[3]. BMS-754807 (0.25 and 0.5 μM) reduces the activated IGF-IR/IR (pIGF-IR/IR), causes a concurrent decrease in phosphorylated AKT in both lung cancer cell lines. BMS-754807 (0.5 μM) also reduces wound closure of lung cancer cells and reduces the ERK phosphorylation. BMS-754807 reduces cell viability in both A549 and NCI-H358 cells, with IC50 of 1.08 μM and 76 μM, respectively[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
BMS-754807 (3.125 and 12.5 mg/kg, p.o.) inhibits tumor growth in IGF-1R-Sal tumor-bearing nude mice. BMS-754807 inhibits tumor growth in a selected group of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3), and mesenchymal (RD1 and Rh41) xenograft tumor models with TGI ranging from 53% to 115%. BMS-754807 is effective at a dose level of 3.125 mg/kg twice daily and as low as 6.25 mg/kg once daily, in the highly sensitive Rh41 rhabdomyosarcoma. BMS-754807 (25 mg/kg) also shows synergy when combined with targeted agents in human tumor cell lines and human xenograft models[1]. Furthmore, BMS-754807 is active at doses from 3 mg/kg upward in the IGF-Sal tumor model[2]. BMS-754807 (25 mg/kg, p.o.) induces significant differences in EFS distribution compared to controls in 18 of 32 evaluable solid tumor xenografts (56%) tested, but in none of the ALL xenografts studied[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Essai clinique |
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Masse moléculaire |
461.49 |
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Formule |
C23H24FN9O |
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CAS No. |
1001350-96-4 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
FC1=CC=C(NC([C@@]2(C)N(C(N=C3NC4=NNC(C5CC5)=C4)=NN6C3=CC=C6)CCC2)=O)C=N1 |
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Livraison | Room temperature in continental US; may vary elsewhere. |
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Stockage |
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Solvant et solubilité |
In Vitro:
DMSO : ≥ 100 mg/mL (216.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%
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Saline
The co-solvents required include: DMSO,
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, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
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Method for preparing stock solution:
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The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
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Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Pureté et documentation | |||||||||||||
Références |
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Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.1669 mL | 10.8345 mL | 21.6689 mL | 54.1724 mL |
5 mM | 0.4334 mL | 2.1669 mL | 4.3338 mL | 10.8345 mL | |
10 mM | 0.2167 mL | 1.0834 mL | 2.1669 mL | 5.4172 mL | |
15 mM | 0.1445 mL | 0.7223 mL | 1.4446 mL | 3.6115 mL | |
20 mM | 0.1083 mL | 0.5417 mL | 1.0834 mL | 2.7086 mL | |
25 mM | 0.0867 mL | 0.4334 mL | 0.8668 mL | 2.1669 mL | |
30 mM | 0.0722 mL | 0.3611 mL | 0.7223 mL | 1.8057 mL | |
40 mM | 0.0542 mL | 0.2709 mL | 0.5417 mL | 1.3543 mL | |
50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0834 mL | |
60 mM | 0.0361 mL | 0.1806 mL | 0.3611 mL | 0.9029 mL | |
80 mM | 0.0271 mL | 0.1354 mL | 0.2709 mL | 0.6772 mL | |
100 mM | 0.0217 mL | 0.1083 mL | 0.2167 mL | 0.5417 mL |