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RUNX1/ETO tetramerization-IN-1 

Cat. No.: HY-151411
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RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model.

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RUNX1/ETO tetramerization-IN-1 Chemical Structure

RUNX1/ETO tetramerization-IN-1 Chemical Structure

CAS No. : 88755-39-9

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Description

RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model[1][2][3].

IC50 & Target

IC50: 630 μM (RUNX1-NHR2 tetramerization)[1]

In Vitro

RUNX1/ETO is composed by the DNA-binding Runt-domain5, the product of the RUNX1 gene, and by four nervy homology regions (NHR1-4), the product of the ETO gene. The NHR2 domain is responsible for the tetramerization of RUNX1/ETO.
RUNX1/ETO tetramerization-IN-1 (compound 7.44) (1 μM and 10 μM; 3, 5, 7 d) selectively reduces the viability of RUNX1/ETO-dependent human leukemic SKNO-1 cells instead of U937 cells[1].
RUNX1/ETO tetramerization-IN-1 (compound 7.44) (25 μM and 50 μM; 5 d) inhibits the growth of and induces myeloid differentiation in RUNX1/ETO-expressing cells (SKNO-1, Kasumi-1, and K562)[2].
RUNX1/ETO tetramerization-IN-1 (100 μM; 7 d) induces growth-arrest and differentiation of RUNX1/ETOtr-expressing CD34+ progenitor cells[2].
RUNX1/ETO tetramerization-IN-1 (compound 7.44) has favorable physicochemical and ADME properties with high aqueous solubility, high stability in buffer and plasma, and a low hepatic intrinsic clearance in vitro, with the aqueous solubility of 60 μg/mL[3].
RUNX1/ETO tetramerization-IN-1 (1 μM and 10 μM) shows a potential to inhibit CYP2B6, 2C9, 2C19, and 3A4[3].
RUNX1/ETO tetramerization-IN-1 (compound 8) (50 μM; 16 h) inhibits c-Jun N-terminal kinase (JNK) and affect the JNK-pathway in cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: RUNX1/ETO-dependent human leukemic SKNO-1 and U937 cells
Concentration: 1 μM and 10 μM
Incubation Time: 3, 5, 7 days
Result: Inhibited the SKNO-1 cell growth specifically.

Cell Viability Assay[3]

Cell Line: Pharmacokinetic properties of RUNX1/ETO tetramerization-IN-1
Concentration:
Incubation Time:
Result:
Kinetic solubility (99% PBS, 1% DMSO) 177 µM
Plasma protein binding (mouse plasma, 60 min) 98.4%
Plasma stability (mouse plasma, 0–240 min) No degradation
Hepatocyte stability (mouse hepatocytes) 2.5 µL/min/million cells
Chemical stability in PBS (0–4 h) No degradation
In Vivo

RUNX1/ETO tetramerization-IN-1 (compound 7.44) (200-250 μg/kg; i.p.; 5 times per week; 130 d) delays tumor growth of RUNX1/ETO cells in mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG immunodeficient mice (NOD.Cg-Prkdcscid Il2rgtm1WjI/SzJ) injected with Kasumi-1 cells[2]
Dosage: 200-250 μg/Kg
Administration: Intraperitoneal injection; 5 times per week, for 130 days
Result: Reduced the dissemination of leukemic cells, remained 75% mice alive at day 130 post-treatment.
Molecular Weight

342.30

Formula

C18H14O7

CAS No.
SMILES

O=C(C(CC(C1=CC=C2OCOC2=C1)=O)C3=CC=C4OCOC4=C3)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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