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FLT3-IN-3

Catalog No. T11298 CAS 2229050-90-0

FLT3-IN-3 is an effective FLT3 inhibitor, and the IC50s of FLT3 WT and FLT3 D835Y are 13 and 8 nM, respectively.

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FLT3-IN-3, CAS 2229050-90-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 109.00
5 mg	In stock	$ 272.00
10 mg	In stock	$ 455.00
25 mg	In stock	$ 753.00
50 mg	In stock	$ 1,060.00
100 mg	In stock	$ 1,430.00
500 mg	In stock	$ 2,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 292.00

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Purity: 99.97%

Biological Description

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Storage & Solubility Information

Description	FLT3-IN-3 is an effective FLT3 inhibitor, and the IC50s of FLT3 WT and FLT3 D835Y are 13 and 8 nM, respectively.
Targets&IC50	FLT3 (WT):13 nM, FLT3 (D835Y):8 nM
In vitro	FLT3-IN-3 inhibits the proliferation of FLT3-ITD positive MV4-11 and MOLM-13 cell lines very effectively at low nanomolar concentrations (GI50 values 2 and 1 nM, respectively). FLT3-IN-3 (1 nM, 10nM, 100 nM, 1 μM and 10 μM; 72 hours) inhibits the Ba/F3 FLT3-ITD cells with the GI50 of 0.034±0.015 μM, and inhibits the parental Ba/F3 cells with the GI50 value of 1.136±0.389 μM. Concentrations as low as 1 nM are sufficient to block the autophosphorylation of the FLT3 receptor tyrosine kinase at three different tyrosine residues (589, 591, and 842). Moreover, this inhibition suppresses phosphorylation of several downstream targets of FLT3. Notably, FLT3-IN-3 (0.01, 0.1, 1, 10 and 100 nM; 1 hours) abolishes phosphorylation of STAT5 at Y694, which is a direct substrate of the oncogenic FLT3-ITD variant. The second pathway affected is the MAPK cascade: Two key components of this signaling pathway, ERK1/2 (T202/Y204) and MEK1/2 (S217/221), exhibit reduced phosphorylation upon treatment with FLT3-IN-3. FLT3-IN-3 also interfers with PI3K/AKT pathway which is confirmed by reduced phosphorylation of AKT at S473.
In vivo	A single dose of FLT3-IN-3 in mice with subcutaneous MV4-11 xenografts causes sustained inhibition of FLT3 and STAT5 phosphorylation over 48 hours.

Molecular Weight	490.64
Formula	C27H38N8O
CAS No.	2229050-90-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (509.54 mM), Sonification is recommended.

References and Literature

1. Gucký T, et al. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869.

Citations

1. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Angiogenesis related Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Anti-Lung Cancer Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

ATH686 Edicotinib Amuvatinib CCT241736 FLT3-IN-10 Tyrosine kinase-IN-1 BMS-2 CHIR-124

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

FLT3-IN-3 2229050-90-0 Angiogenesis Tyrosine Kinase/Adaptors FLT inhibit Fms like tyrosine kinase 3 FLT-3-IN-3 FLT3 CD135 Inhibitor Cluster of differentiation antigen 135 FLT3IN3 FLT3 IN 3 inhibitor

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