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Cat. No.: HY-187646

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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 K_d 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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Please store the product under the recommended conditions in the Certificate of Analysis.

IACS-9439-Cl Chemical Structure

CAS No.: 2231259-57-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
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Biological Activity

Description

In Vitro

OthersAnti-cancer

Others

IACS-9439-Cl is a derivative of IACS-9439. IACS-9439-Cl (compound 1) (1 μM) is an exquisitely selective CSF1R inhibitor with a K_d 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].

Anti-cancer

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

Innate ImmunityAdaptive ImmunityAnti-cancer

Innate Immunity

Adaptive Immunity

IACS-9439-Cl is a derivative of IACS-9439. IACS-9439-Cl (compound 1) (10-200 mg/kg; oral administration, once daily for 5 consecutive days) exhibits a potent in vivo PK/PD correlation in the PANC02 syngeneic tumor model, with an EMR1 mRNA IC₅₀ of approximately 3 μM and a CD4 mRNA IC₅₀ of approximately 18 μM^[1].

Innate Immunity

Anti-cancer

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.

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Chemical Information

CAS No. 2231259-57-5
Molecular Weight 516.02
Formula C₂₃H₂₆ClN₇O₃S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Czako B, et al. Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R. Journal of medicinal chemistry. 2020 Sep 10;63(17):9888-9911. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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