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Sotuletinib

Catalog No. T6119 CAS 953769-46-5

Synonyms: BLZ945

Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), <1000-fold selective against its closest receptor tyrosine kinase homologs.

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Sotuletinib, CAS 953769-46-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 175.00
50 mg	In stock	$ 228.00
100 mg	In stock	$ 397.00
500 mg	In stock	$ 913.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.82%

Purity: 99.44%

Purity: 98.91%

Purity: 98.83%

Purity: 98.25%

Purity: 97.43%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sotuletinib (BLZ945) is an orally active, effective and specific CSF-1R inhibitor (IC50: 1 nM), >1000-fold selective against its closest receptor tyrosine kinase homologs.
Targets&IC50	CSF1R:1 nM
In vitro	In bone marrow-derived macrophages (BMDMs), BLZ945 specifically inhibits CSF-1-dependent proliferation with EC50 of 67 nM, and decreases CSF-1R phosphorylation. BLZ945 blocks the reciprocal effects between macrophages and glioma cells on the survival, proliferation and/ or polarization of each other to promote tumorigenesis. [1]
In vivo	In glioma-bearing mice, BLZ945 blocks tumor progression and significantly improves survival via CSF-1R inhibition. BLZ945 also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. [1] BLZ945 (200 mg/kg, p.o.) decreases the growth of malignant cells in both mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis and keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. [2]
Kinase Assay	Inhibition of biochemical TrkA, TrkB and TrkC: TrkA and TrkC biochemical assays are carried out by HTRF method. The reaction mixtures contains 1 μM peptide substrate, 1 μM ATP, and either 1.8 nM TrkA or 34 nM TrkC in the reaction buffer (50 mM HEPES pH 7.1, 10 mM MgCl2, 2 mM MnCl2, 0.01% BSA, 2.5 mM DTT and 0.1 mM Na3VO4) at a final volume of 10 μL. All reactions are carried out at room temperature in white ProxiPlate? 384-well Plus plates and are quenched with 5 μL of 0.2 mM EDTA at 60 min. Five μL of the detection reagents (2.5 ng PT66K and 0.05 μg SAXL per well) are added, the plates are incubated at room temperature for 1 h and then read in EnVision reader. Compounds are diluted into assay mixture (final DMSO 0.5%), and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions. TrkB biochemical assay is carried out by caliper microfluidic method. The reaction mixtures contained 1 μM peptide substrate, 10 μM ATP, and 2 nM TrkB in a reaction buffer containing 100 mM HEPES, pH 7.5, 5 mM MgCl2, 0.01% Triton X-100, 0.1% BSA, 1 mM DTT, 10 μΜNa3VO4, and 10 μΜBeta-Glycerophosphate. The reactions are carried out at room temperature for 3 hrs, and the products are determined by Caliper EZ-reader. Compounds are diluted into assay mixture (final DMSO 1%), and IC50 values are determined by 12-point (from 50 to 0.000282 μΜ) inhibition curves in duplicate under the assay conditions.
Cell Research	Cell growth rate is determined using the MTT cell proliferation kit. Briefly, cells are plated in triplicate in 96-well plates: 1,000 cells per well for glioma cell lines, 5 x 1,000 cells per well for BMDM and CRL-2467, and 2.5 x 1,000 cells per well for HUVEC and HBMEC cell lines. For all experiments, media is changed every 48 h. Cells are grown in the presence or absence of 6.7–6,700 nM of BLZ945, or 8 μg/mL of CSF-1R neutralizing antibody. BMDM and CRL-2467 cells were supplemented with 10 ng/mL and 30 ng/ mL recombinant mouse CSF-1, respectively. Reduction of the MTT substrate is detected by colorimetric analysis using a plate reader as per the manufacturer's protocol, and measured at 595 nm and 750 nm on a spectraMax 340pc plate reader.(Only for Reference)

Synonyms	BLZ945
Molecular Weight	398.48
Formula	C20H22N4O3S
CAS No.	953769-46-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 73 mg/mL (183.2 mM)

Ethanol: 3 mg/mL (7.52 mM), Heating is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Pyonteck SM, et al. Nat Med. 2013, 19(10), 1264-1272. 2. Strachan DC, et al. Oncoimmunology. 2013, 2(12), e26968. 3. Fan K, Li Y, Wang H, et al. Stress-Induced Metabolic Disorder in Peripheral CD4+ T Cells Leads to Anxiety-like Behavior[J]. Cell. 2019, 179(4): 864-879. e19.

Citations

1. Fan K, Li Y, Wang H, et al. Stress-Induced Metabolic Disorder in Peripheral CD4+ T Cells Leads to Anxiety-like Behavior. Cell. 2019, 179(4): 864-879. e19. 2. Huang C, Ou R, Chen X, et al. Tumor cell-derived SPON2 promotes M2-polarized tumor-associated macrophage infiltration and cancer progression by activating PYK2 in CRC. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-17. 3. Haydar D, Ibañez-Vega J, Crawford J C, et al.CAR T-cell design-dependent remodeling of the brain tumor-immune microenvironment modulates tumor-associated macrophages and anti-glioma activity.Cancer Research Communications.2023

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library NO PAINS Compound Library CNS-Penetrant Compound Library

Related Products

Related compounds with same targets

Vimseltinib CSF1R-IN-17 OSI-930 c-Fms-IN-3 Pexidartinib PF 477736 PRN1371 Onatasertib

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Keywords

Sotuletinib 953769-46-5 Tyrosine Kinase/Adaptors CSF-1R c-Fms CSF1R CSF-1 receptor inhibit Inhibitor colony stimulating factor 1 receptor BLZ945 BLZ-945 BLZ 945 inhibitor

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