Galunisertib [700874-72-2]
Katalog-Nummer HY-13226-10mg
Size : 10mg
Marke : MedChemExpress
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
Galunisertib Chemische Struktur
CAS. Nr. : 700874-72-2
This product is a controlled substance and not for sale in your territory.
Based on 42 publication(s) in Google Scholar
Beschreibung |
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM. |
IC50 & Target |
IC50: 56 nM (TGF-βRI)[4] |
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In Vitro |
Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Klinische Studie |
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Molekulargewicht |
369.42 |
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Formel |
C22H19N5O |
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CAS. Nr. |
700874-72-2 |
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Unlabeled CAS |
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Appearance |
Solid |
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Color |
White to yellow |
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SMILES |
CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1 |
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Versand | Room temperature in continental US; may vary elsewhere. |
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Speicherung |
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Lösungsmittel & Löslichkeit |
In Vitro:
DMSO : 100 mg/mL (270.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 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:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
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
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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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Reinheit & Dokumentation | |||||||||||||
Verweise |
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.7069 mL | 13.5347 mL | 27.0695 mL | 67.6736 mL |
5 mM | 0.5414 mL | 2.7069 mL | 5.4139 mL | 13.5347 mL | |
10 mM | 0.2707 mL | 1.3535 mL | 2.7069 mL | 6.7674 mL | |
15 mM | 0.1805 mL | 0.9023 mL | 1.8046 mL | 4.5116 mL | |
20 mM | 0.1353 mL | 0.6767 mL | 1.3535 mL | 3.3837 mL | |
25 mM | 0.1083 mL | 0.5414 mL | 1.0828 mL | 2.7069 mL | |
30 mM | 0.0902 mL | 0.4512 mL | 0.9023 mL | 2.2558 mL | |
40 mM | 0.0677 mL | 0.3384 mL | 0.6767 mL | 1.6918 mL | |
50 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3535 mL | |
60 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1279 mL | |
80 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8459 mL | |
100 mM | 0.0271 mL | 0.1353 mL | 0.2707 mL | 0.6767 mL |