2. Protein Tyrosine Kinase/RTK
  3. PDGFR c-Fms c-Kit
  4. Seralutinib

Seralutinib  (Synonyms: GB002; PK10571)

Cat. No.: HY-109190 Purity: 99.94%
COA Handling Instructions

Molarity Calculator

Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.

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

Seralutinib Chemical Structure

Seralutinib Chemical Structure

CAS No. : 1619931-27-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 124 In-stock
Solution
10 mM * 1 mL in DMSO USD 124 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 180 In-stock
25 mg USD 320 In-stock
50 mg USD 420 In-stock
100 mg USD 670 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Seralutinib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Seralutinib

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PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension[1][2].

IC50 & Target[2]

PDGFRα

 

PDGFRβ

 

CSF1R

8 nM (IC50)

c-KIT

14 nM (IC50)

In Vivo

Seralutinib (GB002) (two-week treatment, delivered by inhalation) significantly reduces right ventricular systolic pressure and mean pulmonary artery pressure. Hemodynamic changes are accompanied by reduced pulmonary arteriole muscularization and restoration of BMPR2 protein expression in the lung lobes in Seralutinib (GB002)-treated animals. Seralutinib (GB002) is well tolerated[1].
Seralutinib-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation[2].
Seralutinib dose- and time-dependently induces lung BMPR2 protein expression[2].

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

469.53

Formula

C27H27N5O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC(C)=CN=C1)NC2=CC=CC([C@@H](NC3=NC(C4=CC=C(OC)C(OC)=C4)=CN=C3)C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (425.96 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 2.1298 mL 10.6489 mL 21.2979 mL
5 mM 0.4260 mL 2.1298 mL 4.2596 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5.75 mg/mL (12.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.94%

COA (244 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1298 mL 10.6489 mL 21.2979 mL 53.2447 mL
5 mM 0.4260 mL 2.1298 mL 4.2596 mL 10.6489 mL
10 mM 0.2130 mL 1.0649 mL 2.1298 mL 5.3245 mL
15 mM 0.1420 mL 0.7099 mL 1.4199 mL 3.5496 mL
20 mM 0.1065 mL 0.5324 mL 1.0649 mL 2.6622 mL
25 mM 0.0852 mL 0.4260 mL 0.8519 mL 2.1298 mL
30 mM 0.0710 mL 0.3550 mL 0.7099 mL 1.7748 mL
40 mM 0.0532 mL 0.2662 mL 0.5324 mL 1.3311 mL
50 mM 0.0426 mL 0.2130 mL 0.4260 mL 1.0649 mL
60 mM 0.0355 mL 0.1775 mL 0.3550 mL 0.8874 mL
80 mM 0.0266 mL 0.1331 mL 0.2662 mL 0.6656 mL
100 mM 0.0213 mL 0.1065 mL 0.2130 mL 0.5324 mL
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Seralutinib 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:

Seralutinib1619931-27-9GB002 PK10571GB 002GB-002PK10571PK 10571PK-10571PDGFRc-Fmsc-KitPlatelet-derived growth factor receptorCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RSCFRCD117PulmonaryarterialhypertensionPAHInhibitorinhibitorinhibit

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