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RUNX1/ETO tetramerization-IN-1

Catalog No. T61098 CAS 88755-39-9

RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor that specifically targets NHR2 of RUNX1/ETO, effectively inhibiting the tetramerization process. With an EC50 value of 0.25 μM, this compound successfully restores gene expression that has been down-regulated by RUNX1/ETO. Furthermore, RUNX1/ETO tetramerization-IN-1 demonstrates promising anti-leukemic activity by inhibiting the proliferation of SKNO-1 cells dependent on RUNX1/ETO and significantly reducing RUNX1/ETO-associated tumor growth in a mouse model [1] [2] [3].

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RUNX1/ETO tetramerization-IN-1 Chemical Structure

RUNX1/ETO tetramerization-IN-1, CAS 88755-39-9

Pack Size	Availability	Price/USD
2 mg	5 days	$ 337.00
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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Description	RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor that specifically targets NHR2 of RUNX1/ETO, effectively inhibiting the tetramerization process. With an EC50 value of 0.25 μM, this compound successfully restores gene expression that has been down-regulated by RUNX1/ETO. Furthermore, RUNX1/ETO tetramerization-IN-1 demonstrates promising anti-leukemic activity by inhibiting the proliferation of SKNO-1 cells dependent on RUNX1/ETO and significantly reducing RUNX1/ETO-associated tumor growth in a mouse model [1] [2] [3].
In vitro	RUNX1/ETO, comprising the RUNX1 gene's DNA-binding Runt-domain5 and the ETO gene's four nervy homology regions (NHR1-4), is notable for its NHR2 domain, which facilitates tetramerization. RUNX1/ETO tetramerization-IN-1 (compound 7.44) at various concentrations (1 μM and 10 μM over 3, 5, 7 days; 25 μM and 50 μM over 5 days; and 100 μM over 7 days) has been shown to selectively diminish the viability and inhibit the growth, besides inducing differentiation, of RUNX1/ETO-dependent human leukemic cells (specifically SKNO-1, Kasumi-1, and K562 cells) and RUNX1/ETO^tr-expressing CD34+ progenitor cells while showing no significant effect on U937 cells. Furthermore, this compound, with favorable physicochemical and ADME (Absorption, Distribution, Metabolism, and Excretion) properties, including high aqueous solubility (60 μg/mL), stability in buffer and plasma, and low hepatic intrinsic clearance, not only demonstrates inhibition of critical cytochrome P450 enzymes (CYP2B6, 2C9, 2C19, and 3A4) but also inhibits the c-Jun N-terminal kinase (JNK) pathway at 50 μM over 16 hours. These findings underscore its potential as a targeted therapeutic agent in treating RUNX1/ETO-dependent leukemia, supported by cell viability assays and pharmacokinetic studies that reveal its significant stability, potent plasma protein binding, and negligible degradation in physiological conditions.
In vivo	Compound 7.44 (RUNX1/ETO tetramerization-IN-1) administered at a dosage of 200-250 μg/kg via intraperitoneal injection five times weekly for 130 days significantly delays tumor growth in mice inoculated with RUNX1/ETO cells. This regimen resulted in a notable reduction in leukemic cell dissemination and ensured 75% survival in NSG immunodeficient mice (NOD.Cg-Prkdc scid Il2rg tm1WjI /SzJ) injected with Kasumi-1 cells at the end of the treatment period.

Molecular Weight	342.3
Formula	C18H14O7
CAS No.	88755-39-9

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

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RUNX1/ETO tetramerization-IN-1 88755-39-9 inhibitor inhibit

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