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Seralutinib (GB002) PDGFR inhibitor

Cat.No.E0050

Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively.

Chemical Structure

Molecular Weight: 469.54

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: E005001 DMSO]94 mg/mL]false]Ethanol]94 mg/mL]false]Water]Insoluble]false Purity: 99.82%

99.82

Related Targets	EGFR VEGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
Related Products	Crenolanib CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932

Chemical Information, Storage & Stability

Molecular Weight	469.54	Formula	C₂₇H₂₇N₅O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1619931-27-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PK10571			Smiles	COC1=C(OC)C=C(C=C1)C2=CN=CC(=N2)NC(C)C3=CC(=CC=C3)NC(=O)C4=CN=CC(=C4)C

Solubility

In vitro
Batch:

DMSO : 94 mg/mL ( (200.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 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.

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	PDGFRα ^[1] (Cell-free assay) 8 nM PDGFRβ ^[1] (Cell-free assay) 10 nM
References	https://erj.ersjournals.com/content/56/suppl_64/3550

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03926793	Completed	Pulmonary Arterial Hypertension	GB002 Inc. a wholly owned subsidiary of Gossamer Bio Inc.\|Gossamer Bio Inc.	February 4 2020	Phase 1
NCT03473236	Completed	Safety Issues	GB002 Inc. a wholly owned subsidiary of Gossamer Bio Inc.\|Pulmokine Inc.\|Worldwide Clinical Trials\|Gossamer Bio Inc.	September 6 2017	Phase 1

Tech Support

Handling Instructions

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