IACS-9439-Cl
IACS-9439-Cl is a derivative of IACS-9439. IACS-9439 is an orally active and selective colony-stimulating factor 1 receptor (CSF1R) inhibitor with a Kd of 1 nM. IACS-9439-Cl reduces the population of tumor-associated macrophages. IACS-9439-Cl promotes the polarization of macrophages toward the M1 anti-tumor phenotype and decreases the M2 pro-tumor phenotype, thereby exerting a tumor growth inhibitory effect. IACS-9439-Cl can be used in cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 2231259-57-5
- Formula: C23H26ClN7O3S
- Molecular Weight:516.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
IACS-9439-Cl is a derivative of IACS-9439. IACS-9439-Cl (compound 1) (1 μM) is an exquisitely selective CSF1R inhibitor with a Kd of 1 nM for CSF1R, exhibiting greater than 450-fold selectivity against all tested related type III receptor tyrosine kinases[1].
IACS-9439-Cl is a derivative of IACS-9439. IACS-9439-Cl potently inhibits cellular CSF1R autophosphorylation in stimulated THP-1 human monocytic cells, with an IC50 of 17 nM[1].
IACS-9439-Cl is a derivative of IACS-9439. IACS-9439-Cl shows 150-fold cellular selectivity for CSF1R over PDGFRβ in stimulated HEK293/PDGFRβ cells, with a phospho-PDGFRβ IC50 of 3560 nM[1].
IACS-9439-Cl is a derivative of IACS-9439. IACS-9439-Cl potently blocks mCSF1-dependent proliferation of MNSF-60 myelogenous leukemia cells, with an IC50 of 7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
IACS-9439-Cl is a derivative of IACS-9439. IACS-9439 (10-200 mg/kg; oral administration; once daily; for 10 days) drives dose-dependent polarization of tumor-associated macrophages from the pro-tumor M2 phenotype to the anti-tumor M1 phenotype, and exerts potent tumor growth inhibition in the MC38 syngeneic tumor model at a daily dose of 200 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2231259-57-5
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Molecular Weight 516.02
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Formula C23H26ClN7O3S
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SMILES
O(C)C1=C2C(SC(N[C@@H]3[C@@H](O)CCCC3)=N2)=C(Cl)C(OCC4=NC(NC5=CN(C)N=C5)=NC=C4)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IACS-9439-Cl Related Classifications
HY-187646 Related Classifications
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