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.
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. Further protocols information, click here.
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.
Protocols
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)