1. Protein Tyrosine Kinase/RTK Apoptosis TGF-beta/Smad Stem Cell/Wnt
  2. IGF-1R c-Myc Apoptosis TGF-beta/Smad
  3. BTYNB

BTYNB is a structure-specific nucleic acid binder and IGF2BP1 inhibitor (with an IC50 of 5 μM against hBTYNB). BTYNB disrupts the IGF2BP1-RNA interaction and blocks its binding to oncogenic mRNAs such as c-Myc, MDM2, PD-L1. BTYNB completely blocks the INHBA-Smad2/3 pathway, disrupts the MYCN/IGF2BP1 loop, and thereby induces apoptosis and cell cycle arrest, effectively inhibiting the proliferation and survival of cancer cells. In addition, BTYNB acts as an immune activator and tumor microenvironment modulator, enhances T cell-mediated tumor killing, and produces significant synergistic effects with inhibitors of PD-1, BRD and BIRC5. BTYNB can be used in relevant research on various malignant tumors including ovarian cancer, neuroblastoma, leukemia and melanoma.

For research use only. We do not sell to patients.

BTYNB

BTYNB Chemical Structure

CAS No. : 304456-62-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BTYNB is a structure-specific nucleic acid binder and IGF2BP1 inhibitor (with an IC50 of 5 μM against hBTYNB). BTYNB disrupts the IGF2BP1-RNA interaction and blocks its binding to oncogenic mRNAs such as c-Myc, MDM2, PD-L1. BTYNB completely blocks the INHBA-Smad2/3 pathway, disrupts the MYCN/IGF2BP1 loop, and thereby induces apoptosis and cell cycle arrest, effectively inhibiting the proliferation and survival of cancer cells. In addition, BTYNB acts as an immune activator and tumor microenvironment modulator, enhances T cell-mediated tumor killing, and produces significant synergistic effects with inhibitors of PD-1, BRD and BIRC5. BTYNB can be used in relevant research on various malignant tumors including ovarian cancer, neuroblastoma, leukemia and melanoma[1][2][3][4][5].

IC50 & Target

IC50: 5 μM (IMP1 c-Myc mRNA internation)[1]

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
21.56 μM
Compound: 2; BTYNB
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 38382391]
K562 IC50
6.76 μM
Compound: 2; BTYNB
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 38382391]
In Vitro

BTYNB (20 μM; 24-36 h) significantly inhibits the migration and invasion of KYSE30 and TE1 ESCC cells in vitro[2].
BTYNB (10 μM; 48 h) significantly increases apoptosis in KYSE30 and TE1 ESCC cells[2].
BTYNB (0.38-24 µM; 72 h) combined with Mivebresib exhibits strong synergy in reducing BE(2)-C human neuroblastoma cell viability after 72 hours of treatment[3].
BTYNB (7-21 μM; 24 h) induces mild apoptosis in human HL60 and K562 leukemic cells after 24 h of treatment, accompanied by significant upregulation of the pro-apoptotic gene BAK[4].
BTYNB (7-21 μM; 24 h) induces S-phase cell cycle arrest in human K562 leukemic cells (with no effect on HL60 cells) after 24 h of treatment, accompanied by significant upregulation of the cell cycle arrest gene p21 in both cell lines[4].

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

Cell Migration Assay [2]

Cell Line: KYSE30, TE1 esophageal squamous cell carcinoma (ESCC) cells
Concentration: 20 μM
Incubation Time: 36 h (KYSE30 cells); 24 h (TE1 cells)
Result: Reduced the relative cell area covered by invading KYSE30 cells to approximately 30% of control levels.
Reduced the relative cell area covered by migrating KYSE30 cells to approximately 40% of control levels.
Reduced the relative cell area covered by invading TE1 cells to approximately 20% of control levels.
Reduced the relative cell area covered by migrating TE1 cells to approximately 10% of control levels.
In Vivo

Combination of BTYNB (40 mg/kg; i.p.; twice weekly) with anti-PD-1 blockade therapy significantly improves the median survival of mice, reduces tumor cell burden, and converts the tumor microenvironment to a more immunoresponsive state[1].

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

Animal Model: C57BL/6NCrl mice (female, 6 weeks old, intraperitoneal injection of 5 × 106 ID8/Trp53-/- cells)[1]
Dosage: 40 mg/kg (monotherapy); 40 mg/kg (combination with anti-PD-1 antibody 8 mg/kg)
Administration: i.p.; twice weekly
Result: Improved median survival by ~30% compared to the control group and by 15% compared to anti-PD-1 monotherapy when combined with anti-PD-1 antibody.
Reduced tumor cell dominance in ascitic fluid to 67% when combined with anti-PD-1 antibody.
Shifted tumor cells to an immune-responsive phenotype when combined with anti-PD-1 antibody.
Increased immune cell accumulation in ascites (with a higher proportion of cytotoxic T cells than BTYNB monotherapy) when combined with anti-PD-1 antibody.
Molecular Weight

309.18

Formula

C12H9BrN2OS

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=CC=C1/N=C/C2=CC=C(S2)Br)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (202.15 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 3.2344 mL 16.1718 mL 32.3436 mL
5 mM 0.6469 mL 3.2344 mL 6.4687 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume (start)

V1

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Concentration (final)

C2

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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 (8.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (8.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

Purity: 98.0%

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 (protect from light). 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 3.2344 mL 16.1718 mL 32.3436 mL 80.8590 mL
5 mM 0.6469 mL 3.2344 mL 6.4687 mL 16.1718 mL
10 mM 0.3234 mL 1.6172 mL 3.2344 mL 8.0859 mL
15 mM 0.2156 mL 1.0781 mL 2.1562 mL 5.3906 mL
20 mM 0.1617 mL 0.8086 mL 1.6172 mL 4.0430 mL
25 mM 0.1294 mL 0.6469 mL 1.2937 mL 3.2344 mL
30 mM 0.1078 mL 0.5391 mL 1.0781 mL 2.6953 mL
40 mM 0.0809 mL 0.4043 mL 0.8086 mL 2.0215 mL
50 mM 0.0647 mL 0.3234 mL 0.6469 mL 1.6172 mL
60 mM 0.0539 mL 0.2695 mL 0.5391 mL 1.3477 mL
80 mM 0.0404 mL 0.2021 mL 0.4043 mL 1.0107 mL
100 mM 0.0323 mL 0.1617 mL 0.3234 mL 0.8086 mL
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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.

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