Sotuletinib [953769-46-5]
Cat# HY-12768-100mg
Size : 100mg
Brand : MedChemExpress
BLZ945 est un CSF-1R (c-Fms) inhibiteur puissant, sélectif et cerveau-pénétrant avec un IC50 de 1 nM, montrant plus 1 000 fois de sélectivité par rapport à ses homologues récepteurs tyrosine kinase les plus proches.
Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
For research use only. We do not sell to patients.
Sotuletinib Chemical Structure
CAS No. : 953769-46-5
This product is a controlled substance and not for sale in your territory.
Based on 17 publication(s) in Google Scholar
Other Forms of Sotuletinib:
- Sotuletinib hydrochloride In-stock
- Sotuletinib dihydrochloride Get quote
Description |
Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs[1]. |
IC50 & Target |
IC50: 1 nM (CSF-1R), 3.2 μM (c-Kit), 4.8 μM (PDGFRβ), 9.1 μM (Flt3)[1] |
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In Vitro |
Treatment of bone marrow-derived macrophages (BMDMs) with Sotuletinib inhibits CSF-1-dependent proliferation (EC50=67 nM), and decreases CSF-1R phosphorylation, similar to CSF-1R antibody blockade. Sotuletinib also reduces viability of CRL-2467 microglia, Ink4a/Arf?/? BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, Sotuletinib treatment in culture does not affect proliferation of any PDG-derived tumor cell lines (all Csf-1r-negative), or U-87 MG human glioma cells, and PDG cell tumor sphere formation is unaffected. Thus, Sotuletinib has no direct effects on glioma cells, and perturbs macrophage survival through CSF-1R inhibition[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Mice are treated with Sotuletinib or vehicle, and evaluated for symptom-free survival. Median survival in the vehicle-treated cohort is 5.7 weeks. In striking contrast, Sotuletinib significantly improves long-term survival. This endpoint is chosen because Ink4a/Arf?/? mice develop spontaneous tumors, including lymphomas and sarcomas, beginning at ~30 weeks. Sotuletinib is well-tolerated over long-term treatment, with no visible side-effects, consistent with histopathological studies. Histological grading revealed high-grade, invasive gliomas in all vehicle-treated mice. By contrast, Sotuletinib-treated animals have significantly less-malignant tumors, and no detectable lesions in 55.6% of asymptomatic mice at the endpoint[1]. Mice receiving Sotuletinib shows reduced CSF1R staining in both cervical tumors and the associated stroma, with a significant decrease in CSF1R+ stromal macrophages relative to vehicle-treated mice (P<0.05)[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
398.48 |
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Formula |
C20H22N4O3S |
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CAS No. |
953769-46-5 |
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Appearance |
Solid |
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Color |
Off-white to light brown |
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SMILES |
O=C(C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1)NC |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 83.33 mg/mL (209.12 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:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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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Purity & Documentation |
Purity: 99.78% |
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References |
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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 | 2.5095 mL | 12.5477 mL | 25.0954 mL | 62.7384 mL |
5 mM | 0.5019 mL | 2.5095 mL | 5.0191 mL | 12.5477 mL | |
10 mM | 0.2510 mL | 1.2548 mL | 2.5095 mL | 6.2738 mL | |
15 mM | 0.1673 mL | 0.8365 mL | 1.6730 mL | 4.1826 mL | |
20 mM | 0.1255 mL | 0.6274 mL | 1.2548 mL | 3.1369 mL | |
25 mM | 0.1004 mL | 0.5019 mL | 1.0038 mL | 2.5095 mL | |
30 mM | 0.0837 mL | 0.4183 mL | 0.8365 mL | 2.0913 mL | |
40 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5685 mL | |
50 mM | 0.0502 mL | 0.2510 mL | 0.5019 mL | 1.2548 mL | |
60 mM | 0.0418 mL | 0.2091 mL | 0.4183 mL | 1.0456 mL | |
80 mM | 0.0314 mL | 0.1568 mL | 0.3137 mL | 0.7842 mL | |
100 mM | 0.0251 mL | 0.1255 mL | 0.2510 mL | 0.6274 mL |
Sotuletinib Related Classifications
- Protein Tyrosine Kinase/RTK
- c-Fms