1. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling
  2. SHP1 STAT
  3. BCI-137

BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8+ T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields.

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BCI-137

BCI-137 Chemical Structure

CAS No. : 112170-24-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8+ T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields[1].

IC50 & Target

STAT1

 

In Vitro

BCI-137 (5-10 μM) concentration-dependently enhances STAT1 activation induced by 20 ng/mL IFN-γ in both human bladder cancer cell line UMUC-3 and SYBC1, and reduces the expression of PTPN6[1].

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

Western Blot Analysis[1]

Cell Line: Human bladder cancer cell line UMUC-3 and SYBC1
Concentration: 5 μM, 10 μM
Incubation Time: 24 h; stimulated with 20 ng/mL IFN-γ
Result: Dose dependently enhances STAT1 activation induced by 20 ng/mL IFN-γ in human bladder cancer cell line UMUC-3, and reduces the expression of PTPN6
In Vivo

BCI-137 (100 mg/kg; intermittently; 4 doses every 3 days beginning on day 7) in combination with anti-PD-1 antibody significantly reduces subcutaneous MB49 bladder cancer tumor volume, enhances CD8+ T cell infiltration and effector function in tumors, and prolongs mouse survival[1].

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

Animal Model: C57BL/6 mice with Bladder cancer (6-8-week-old female, subcutaneous MB49 bladder cancer cell-induced model)[1]
Dosage: 100 mg/kg
Administration: Intermittently; 4 doses every 3 days beginning on day 7
Result: Significantly reduced subcutaneous MB49 tumor volume at day 19 when combined with anti-PD-1 antibody.
Increased the percentage of CD8+ T cells infiltrating tumors when combined with anti-PD-1 antibody.
Elevated the percentage of IFN-γ+/CD8+ T cells in tumors when combined with anti-PD-1 antibody.
Elevated the percentage of TNF-α+/CD8+ T cells in tumors when combined with anti-PD-1 antibody.
Prolonged overall mouse survival.
Molecular Weight

313.29

Formula

C11H11N3O6S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C(O)=O)NS(=O)(C1=CC2=C(C=C1)NC(C(N2)=O)=O)=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 (319.19 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 3.1919 mL 15.9597 mL 31.9193 mL
5 mM 0.6384 mL 3.1919 mL 6.3839 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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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 (7.98 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 (7.98 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

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(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

Purity: 99.84%

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 3.1919 mL 15.9597 mL 31.9193 mL 79.7983 mL
5 mM 0.6384 mL 3.1919 mL 6.3839 mL 15.9597 mL
10 mM 0.3192 mL 1.5960 mL 3.1919 mL 7.9798 mL
15 mM 0.2128 mL 1.0640 mL 2.1280 mL 5.3199 mL
20 mM 0.1596 mL 0.7980 mL 1.5960 mL 3.9899 mL
25 mM 0.1277 mL 0.6384 mL 1.2768 mL 3.1919 mL
30 mM 0.1064 mL 0.5320 mL 1.0640 mL 2.6599 mL
40 mM 0.0798 mL 0.3990 mL 0.7980 mL 1.9950 mL
50 mM 0.0638 mL 0.3192 mL 0.6384 mL 1.5960 mL
60 mM 0.0532 mL 0.2660 mL 0.5320 mL 1.3300 mL
80 mM 0.0399 mL 0.1995 mL 0.3990 mL 0.9975 mL
100 mM 0.0319 mL 0.1596 mL 0.3192 mL 0.7980 mL
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Help & FAQs
  • 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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BCI-137
Cat. No.:
HY-119024
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