Sotuletinib (Synonyms: BLZ945)

Name: Sotuletinib
Brand: MedChemExpress
SKU: HY-12768
Rating: 5.0 (23 reviews)

Cat. No.: HY-12768 Purity: 99.80% ee.: 100.00%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC₅₀ of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.

For research use only. We do not sell to patients.

Sotuletinib Chemical Structure

CAS No. : 953769-46-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Sotuletinib:

Sotuletinib hydrochloride Get quote
Sotuletinib dihydrochloride Get quote

23 Publications Citing Use of MCE Sotuletinib

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 1 nM (CSF-1R), 3.2 μM (c-Kit), 4.8 μM (PDGFRβ), 9.1 μM (Flt3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Panc02	IC₅₀	18 μM Compound: BLZ945	Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in EMR1 F4/80 mRNA expression after 5 days Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in EMR1 F4/80 mRNA expression after 5 days	[PMID: 32787110]
Panc02	IC₅₀	56 μM Compound: BLZ945	Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in CD4 mRNA expression after 5 days Antitumour activity against mouse Panc02 cells implanted in po dosed C57BL/6 mouse assessed as reduction in CD4 mRNA expression after 5 days	[PMID: 32787110]

In Vitro

Treatment of bone marrow-derived macrophages (BMDMs) with Sotuletinib inhibits CSF-1-dependent proliferation (EC₅₀=67 nM), and decreases CSF-1R phosphorylation, similar to CSF-1R antibody blockade. Sotuletinib also reduces viability of CRL-2467 microglia, Ink4a/Arf^/ BMDMs (PDG genetic background), and NOD/SCID BMDMs. Importantly, Sotuletinib treatment in culture does not affect proliferation of any PDG-derived tumor cell lines (all Csf-1r-negative), or U-87 MG human glioma cells, and PDG cell tumor sphere formation is unaffected. Thus, Sotuletinib has no direct effects on glioma cells, and perturbs macrophage survival through CSF-1R inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mice are treated with Sotuletinib or vehicle, and evaluated for symptom-free survival. Median survival in the vehicle-treated cohort is 5.7 weeks. In striking contrast, Sotuletinib significantly improves long-term survival. This endpoint is chosen because Ink4a/Arf^/ mice develop spontaneous tumors, including lymphomas and sarcomas, beginning at ~30 weeks. Sotuletinib is well-tolerated over long-term treatment, with no visible side-effects, consistent with histopathological studies. Histological grading revealed high-grade, invasive gliomas in all vehicle-treated mice. By contrast, Sotuletinib-treated animals have significantly less-malignant tumors, and no detectable lesions in 55.6% of asymptomatic mice at the endpoint^[1]. Mice receiving Sotuletinib shows reduced CSF1R staining in both cervical tumors and the associated stroma, with a significant decrease in CSF1R⁺ stromal macrophages relative to vehicle-treated mice (P<0.05)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

398.48

Formula

C₂₀H₂₂N₄O₃S

CAS No.

953769-46-5

Appearance

Solid

Color

Off-white to light brown

SMILES

O=C(C1=NC=CC(OC2=CC=C3N=C(N[C@H]4[C@H](O)CCCC4)SC3=C2)=C1)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (209.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5095 mL	12.5477 mL	25.0954 mL
5 mM	0.5019 mL	2.5095 mL	5.0191 mL
10 mM	0.2510 mL	1.2548 mL	2.5095 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% SBE-β-CD in Saline
Solubility: 10 mg/mL (25.10 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.80% ee.: 100.00%

Select Batch:

Data Sheet (279 KB) SDS (537 KB)

COA (247 KB) HNMR (297 KB) NP-HPLC (303 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72. [Content Brief]

[2]. Strachan DC, et al. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8+ T cells. Oncoimmunology. 2013 Dec 1;2(12):e26968. [Content Brief]

Cell Assay ^[1]	Cell growth rate is determined using the MTT cell proliferation kit. Briefly, cells are plated in triplicate in 96-well plates: 1×10³ cells per well for glioma cell lines, 5×10³ cells per well for BMDM and CRL-2467, and 2.5×10³ 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 Sotuletinib, or 8 μg/mL of CSF-1R neutralizing antibody. To test the sensitivity to PDGFR inhibition, PDGC lines are cultured in the presence of 10,000 nM STI571 or 10,000 nM PTK787 (diluted from 10 mM stock solutions in DMSO). HUVEC and HBMEC cells are supplemented with ECGF supplied by the manufacturer unless otherwise indicated. Reduction of the MTT substrate is detected by colorimetric analysis using a plate reader as per the manufacturer’s protocol. 10 μL of MTT labeling reagent is added to each well and then incubated for 4 h at 37°C, followed by the addition of 100 μL MTT solubilization reagent overnight. The mixture is gently resuspended and absorbance is measured at 595 nm and 750 nm on a spectraMax 340pc plate reader^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Tumors are measured using calipers and volumes calculated based on the formula: volume=(width)²×length/2. In MMTV-PyMT mouse studies, 56-63 d old female mice are randomized into groups based on tumor volumes and dosed with either 20% Captisol vehicle or 200 mg/kg Sotuletinib. Dosing is administered by oral gavage once daily and tumor volumes are measured twice weekly. 5A1 rat anti-mouse CSF1 neutralizing antibody or rat IgG control is dosed at 10 mg/kg by intraperitoneal injection every 5 d. To calculate pulmonary metastasis in MMTV-PyMT transgenic mice, formalin-fixed paraffin-embedded lungs are serially sectioned and stained with hematoxylin and eosin. Tumor regions are scored by tumor burden (total tumor area divided by total lung area), size (tumor diameter), and according to the total number of individual metastases counted in a single-blind fashion. These values are averaged across the entire depth of the lung to obtain the final value. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Pyonteck SM, et al. CSF-1R inhibition alters macrophage polarization and blocks glioma progression. Nat Med. 2013 Oct;19(10):1264-72. [Content Brief] [2]. Strachan DC, et al. CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8+ T cells. Oncoimmunology. 2013 Dec 1;2(12):e26968. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5095 mL	12.5477 mL	25.0954 mL	62.7384 mL
	5 mM	0.5019 mL	2.5095 mL	5.0191 mL	12.5477 mL
	10 mM	0.2510 mL	1.2548 mL	2.5095 mL	6.2738 mL
	15 mM	0.1673 mL	0.8365 mL	1.6730 mL	4.1826 mL
	20 mM	0.1255 mL	0.6274 mL	1.2548 mL	3.1369 mL
	25 mM	0.1004 mL	0.5019 mL	1.0038 mL	2.5095 mL
	30 mM	0.0837 mL	0.4183 mL	0.8365 mL	2.0913 mL
	40 mM	0.0627 mL	0.3137 mL	0.6274 mL	1.5685 mL
	50 mM	0.0502 mL	0.2510 mL	0.5019 mL	1.2548 mL
	60 mM	0.0418 mL	0.2091 mL	0.4183 mL	1.0456 mL
	80 mM	0.0314 mL	0.1568 mL	0.3137 mL	0.7842 mL
	100 mM	0.0251 mL	0.1255 mL	0.2510 mL	0.6274 mL

Sotuletinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sotuletinib953769-46-5BLZ945BLZ 945BLZ-945c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RInhibitorinhibitorinhibit

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Sotuletinib (Synonyms: BLZ945)

Customer Review

Other Forms of Sotuletinib:

Sotuletinib Related Antibodies

23 Publications Citing Use of MCE Sotuletinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Sotuletinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Sotuletinib Related Classifications

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