Fedratinib hydrochloride hydrate

Modify Date: 2024-01-03 19:58:37

Fedratinib hydrochloride hydrate structure	Common Name	Fedratinib hydrochloride hydrate
	CAS Number	1374744-69-0	Molecular Weight	615.615
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₇H₄₀Cl₂N₆O₄S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Fedratinib hydrochloride hydrate

Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].

Name	UH9J2HBQWJ
Synonym	More Synonyms

Description	Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK
Target	JAK2:3 nM (IC50) JAK2(V617F):3 nM (IC50) Flt3:15 nM (IC50) Ret:48 nM (IC50)
In Vitro	Fedratinib (TG101348) inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC50 value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC50 value of ∼420 nM[1]. Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation[1]. Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner[1].
In Vivo	Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals[1]. Animal Model: C57Bl/6 mice induced by the JAK2V617F mutation[1] Dosage: 60 mg/kg, 120 mg/kg Administration: Oral gavage; twice daily; for 42 days Result: Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.
References	[1]. Wernig G, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008 Apr;13(4):311-20. [2]. Geron I, et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell. 2008 Apr;13(4):321-30.

Molecular Formula	C₂₇H₄₀Cl₂N₆O₄S
Molecular Weight	615.615
Exact Mass	614.220886

Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-, hydrochloride, hydrate (1:2:1)

N-(2-Methyl-2-propanyl)-3-{[5-methyl-2-({4-[2-(1-pyrrolidinyl)ethoxy]phenyl}amino)-4-pyrimidinyl]amino}benzenesulfonamide dihydrochloride hydrate

UH9J2HBQWJ

DC Chemicals Limited
China
Product Name: Fedratinib hydrochloride hydrate
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide hydrochloride hydrate (1:2:1)
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Fedratinib hydrochloride hydrate

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