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ChemicalBook--->CAS DataBase List--->2387765-27-5

2387765-27-5

2387765-27-5 Structure

2387765-27-5 Structure
IdentificationBack Directory
[Name]

JAK2/FLT3-IN-1
[CAS]

2387765-27-5
[Synonyms]

Flonoltinib
JAK2/FLT3-IN-1
JAK2/FLT3 IN 1,JAK-2/FLT3-IN-1,JAK2/FLT3IN1
Ethanol, 2-[[1-[2-fluoro-4-[[5-methyl-4-[1-(1-methylethyl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]phenyl]-4-piperidinyl]methylamino]-
[Molecular Formula]

C25H34FN7O
[MDL Number]

MFCD32263440
[MOL File]

2387765-27-5.mol
[Molecular Weight]

467.59
Chemical PropertiesBack Directory
[Boiling point ]

660.2±65.0 °C(Predicted)
[density ]

1.26±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

14.74±0.10(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib has anti-cancer activity[1].
[in vivo]

Flonoltinib (30 and 60 mg/kg/day; p.o.; for 14 days) exhibits significant antitumor effects[1].

Animal Model:NOD/SCID mouse models[1]
Dosage:30 and 60 mg/kg
Administration:Oral administration; daily; for 14 days
Result:Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.
[IC 50]

JAK2: 0.7 nM (IC50); FLT3: 4 nM (IC50); JAK1: 26 nM (IC50); JAK3: 39 nM (IC50)
[References]

[1] Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31. DOI:10.1021/acs.jmedchem.9b01348
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