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HM43239

Catalog No. T9428 CAS 2294874-49-8

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].

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HM43239, CAS 2294874-49-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 64.00
5 mg	In stock	$ 155.00
10 mg	In stock	$ 238.00
25 mg	In stock	$ 465.00
50 mg	In stock	$ 665.00
100 mg	In stock	$ 928.00
1 mL * 10 mM (in DMSO)	In stock	$ 197.00

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Purity: 98.56%

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Chemical Properties

Storage & Solubility Information

Description	HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].
Targets&IC50	FLT3 (D835Y):1.0 nM, FLT3 (WT):1.1 nM, FLT3 (ITD):1.8 nM
In vitro	HM43239 potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation like MV4-11 (IC 50 : 1.3 nM), MOLM-13 (IC 50 : 5.1 nM), and MOLM-14 (IC 50 : 2.9 nM). Besides, HM43239 inhibits KG1a cells (CD34+/CD38- cells) proliferation [1]. HM43239 induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells) [1]. HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells [3].
In vivo	HM43239 exhibits the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity [1]. HM43239 prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models [3].

Molecular Weight	501.07
Formula	C29H33ClN6
CAS No.	2294874-49-8

Storage

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

Solubility Information

DMSO: 50 mg/mL (99.79 mM)

References and Literature

1. Miyoung Lee, et al. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res July 1 2018 (78) (13 Supplement) 804. 2. Waters S, et al. Preclinical Pharmacology of [2-(3-Fluoro-5-Methanesulfonyl-phenoxy)Ethyl](Propyl)amine (IRL790), a Novel Dopamine Transmission Modulator for the Treatment of Motor and Psychiatric Complications in Parkinson Disease. J Pharmacol Exp Ther. 2020 Jul;374(1):113-125.

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：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Angiogenesis related Compound Library Bioactive Compound Library NO PAINS Compound Library Anti-Cancer Compound Library

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Keywords

HM43239 2294874-49-8 Angiogenesis Tyrosine Kinase/Adaptors FLT HM 43239 HM-43239 inhibitor inhibit

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