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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $172 | In Stock | |
50 mg | $228 | In Stock | |
100 mg | $396 | In Stock | |
200 mg | $578 | In Stock |
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). |
Targets&IC50 | CSF1R (FMS):1 nM |
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.[1] |
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.[2] |
Molecular Weight | 434.94 |
Formula | C20H23ClN4O3S |
Cas No. | 2222138-31-8 |
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 |
Color | White |
Appearance | Solid |
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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80.00 mg/mL (183.93 mM), Sonication is recommended. H2O: 80.00 mg/mL (183.93 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/H2O
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