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Sotuletinib (BLZ945) CSF-1R inhibitor

Name: Sotuletinib (BLZ945)
Brand: Selleck Chemicals
SKU: S7725
Availability: InStock
Rating: 5 (34 reviews)

Cat.No.S7725

Sotuletinib (BLZ945) is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, and it is >1000-fold selective against its closest receptor tyrosine kinase homologs.

Chemical Structure

Molecular Weight: 398.48

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
Related Products	GW2580 PLX5622 Edicotinib(JNJ-40346527) CSF1R-IN-1 Sulfatinib Vimseltinib Ki20227 AZD7507 Cabiralizumab (Anti-CSF1R / M-CSFR / CD115) Chiauranib ARRY-382 Pimicotinib

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
mouse M-NFS-60 cells	Antiproliferative assay				Antiproliferative activity against mouse M-NFS-60 cells harboring CSF1, EC50 = 0.071 μM.	29293000
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	398.48	Formula	C₂₀H₂₂N₄O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	953769-46-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (200.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 5%TWEEN80 3 53%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.600mg/ml (4.02mM)	Taking the 1 mL working solution as an example, add 20 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.860mg/ml (7.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 57.1 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (5.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CSF-1R ^[1] (Cell-free assay) 1 nM
In vitro	In bone marrow-derived macrophages (BMDMs), Sotuletinib (BLZ945) specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. It 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, Sotuletinib (BLZ945) blocks tumor progression and significantly improves survival via CSF-1R inhibition. It also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. ^[1] This compound (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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/24056773/ [2] https://pubmed.ncbi.nlm.nih.gov/24498562/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pCSF1R / tCSF1R / pAKT / tAKT / p-mTOR / mTOR / pERK / ERK / p-NFKB / NFKB / p-P70S6K / P70S6K / Arg-1		30956894

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04066244	Active not recruiting	Amyotrophic Lateral Sclerosis	Novartis Pharmaceuticals\|Novartis	December 30 2019	Phase 2
NCT02829723	Terminated	Advanced Solid Tumors	Novartis Pharmaceuticals\|Novartis	October 21 2016	Phase 1\|Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Does this molecule bind to any neurogenesis inhibiting enzymes? Which of the csf1r inhibitors is the most specific?

Answer:
Its IC50 to CSF1R is about 0.001uM, C-Kit 3.2uM and PDGFR-β 4.8uM. Therefore, it is relatively specific to CSF1R.

Question 2:
We want to deliver it by oral gavage to mice, can you provide some advice about formulation for this compound?

Answer:
It can be dissolved in 0.5% CMC Na+1% Tween 80 at 20 mg/ml as a suspension.

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