Sotuletinib hydrochloride

SKU: orb3027139

Description

Sotuletinib hydrochloride (BLZ945 HCl) is a selective, brain-penetrant CSF-1R (c-Fms) inhibitor (IC50=1 nM), exhibiting 1000-fold greater selectivity than other receptor tyrosine kinase homologues. It elevates liver enzymes and induces Kupffer cell depletion, making it suitable for studying amyotrophic lateral sclerosis (ALS) and metastatic triple-negative breast cancer (TNBC).

Research Area

Signal Transduction

Key Properties

• CAS Number: 2222138-31-8
• MW: 434.94
• Purity: 98.81%
• Formula: C₂₀H₂₃ClN₄O₃S
• SMILES: N(C=1SC=2C(N1)=CC=C(OC=3C=C(C(NC)=O)N=CC3)C2)[C@H]4[C@H](O)CCCC4.Cl
• Target: CSF-1R,c-Fms
• Solubility: DMSO:80 mg/mL (183.93 mM);H2O:80 mg/mL (183.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.59 mM)

Bioactivity

• Target IC50:
  CSF1R (FMS):1 nM
• In Vivo:
  Methods: Sotuletinib hydrochloride (200 mg/kg, once daily) was administered to MMTV-PyMT mice via oral gavage to assess the effects of Sotuletinib hydrochloride on tumor growth, TAMs, and CD8+ T cells. Results: Sotuletinib hydrochloride treatment significantly decreased TAMs and tumor volume while enhancing the infiltration of CD8+ T cells.
• In Vitro:
  Methods: Bone marrow-derived macrophages (BMDMs) were treated with Sotuletinib hydrochloride (67nM-6700nM), and cell proliferation was assessed via MTT assay. Results: Sotuletinib hydrochloride significantly inhibited CSF-1-dependent proliferation and CSF-1R phosphorylation in BMDMs.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CSF-1R,c-Fms