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  4. RUNX1/ETO tetramerization-IN-1

RUNX1/ETO tetramerization-IN-1 

Cat. No.: HY-151411 Purity: 99.88%
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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 374 In-stock
Solution
10 mM * 1 mL in DMSO USD 374 In-stock
Solid
5 mg USD 340 In-stock
10 mg USD 550 In-stock
25 mg USD 1100 In-stock
50 mg USD 1760 In-stock
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Based on 1 publication(s) in Google Scholar

RUNX1/ETO tetramerization-IN-1 Related Antibodies

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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].

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

RUNX1/ETO tetramerization-IN-1 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (292.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9214 mL 14.6071 mL 29.2141 mL
5 mM 0.5843 mL 2.9214 mL 5.8428 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (7.30 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.30 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9214 mL 14.6071 mL 29.2141 mL 73.0354 mL
5 mM 0.5843 mL 2.9214 mL 5.8428 mL 14.6071 mL
10 mM 0.2921 mL 1.4607 mL 2.9214 mL 7.3035 mL
15 mM 0.1948 mL 0.9738 mL 1.9476 mL 4.8690 mL
20 mM 0.1461 mL 0.7304 mL 1.4607 mL 3.6518 mL
25 mM 0.1169 mL 0.5843 mL 1.1686 mL 2.9214 mL
30 mM 0.0974 mL 0.4869 mL 0.9738 mL 2.4345 mL
40 mM 0.0730 mL 0.3652 mL 0.7304 mL 1.8259 mL
50 mM 0.0584 mL 0.2921 mL 0.5843 mL 1.4607 mL
60 mM 0.0487 mL 0.2435 mL 0.4869 mL 1.2173 mL
80 mM 0.0365 mL 0.1826 mL 0.3652 mL 0.9129 mL
100 mM 0.0292 mL 0.1461 mL 0.2921 mL 0.7304 mL
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RUNX1/ETO tetramerization-IN-1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RUNX1/ETO tetramerization-IN-188755-39-9Othersanti-leukemicnervy homology region 2cell proliferationSKNO-1acute myeloid leukemiaAMLInhibitorinhibitorinhibit

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