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Flumatinib (HH-GV-678) Bcr-Abl inhibitor

Cat.No.S9973

Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2  nM, 307.6  nM and 665.5  nM for c-Abl, PDGFRβand c-Kit, respectively.

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Quality Control

Batch: Purity: 99.75%
99.75

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (177.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Chemical Information, Storage & Stability

Molecular Weight 562.59 Formula

C29H29F3N8O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 895519-90-1 -- Storage of Stock Solutions

Synonyms HH-GV678 SMILES CN1CCN(CC1)CC2=CC=C(C=C2C(F)(F)F)C(=O)NC3=CN=C(C)C(=C3)NC4=NC(=CC=N4)C5=CN=CC=C5

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
c-Abl
1.2 nM
PDGFRβ
307.6 nM
c-Kit
665.5 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2022-05-10)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05367765 NOT_YET_RECRUITING
CML, Chronic Phase
Jiangsu Hansoh Pharmaceutical Co., Ltd.
2022-04-30 PHASE4
NCT06530810 NOT_YET_RECRUITING
Chronic Myelogenous Leukemia; CML Chronic Phase; CML Accelerated Phase
Jiangsu Hansoh Pharmaceutical Co., Ltd.
2024-07-31 PHASE1
NCT05433532 COMPLETED
Philadelphia Chromosome; Acute Myeloid Leukemia; Acute Lymphoblastic Leukemia; Chronic Myeloid Leukemia; Mixed Phenotype Acute Leukemia
The First Affiliated Hospital of Soochow University
2022-05-01 PHASE2
NCT04677439 UNKNOWN
Flumatinib; Chronic Myeloid Leukemia, Chronic Phase; Imatinib
Shenzhen Second People's Hospital
2021-01-01 PHASE4
NCT04933526 UNKNOWN
Chronic Myeloid Leukemia in Chronic Phase
Shenzhen Second People's Hospital
2021-07-01 PHASE4
NCT05071482 TERMINATED
Acute Leukemia
Institute of Hematology & Blood Diseases Hospital, China
2021-09-16 PHASE4

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