2. Cell Cycle/DNA Damage
  3. CDK
  4. BI-1347

BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity.

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

BI-1347 Chemical Structure

BI-1347 Chemical Structure

CAS No. : 2163056-91-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

BI-1347 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BI-1347

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity[1][2].

IC50 & Target[1]

CDK8

1.1 nM (IC50)

In Vitro

BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells[2].
BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells[2].

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

BI-1347 Related Antibodies

Western Blot Analysis[2]

Cell Line: Mouse splenic NK cells
Concentration: 150 nM
Incubation Time: 44 hours
Result: Increased the proportion of granzyme B-positive NK cells by approximately 4-fold.

Western Blot Analysis[2]

Cell Line: Human NK92MI cells
Concentration: 0.1 nM-10 μM
Incubation Time: 24 hours
Result: Increased perforin levels with an EC50 value of 7.2 nM.
In Vivo

BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity in vivo[2].
BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model[2].

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

Animal Model: B16-F10-luc2 syngeneic melanoma model[2]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; once daily; 30 d
Result: Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%.
Showed minimal effect on body weight at 10 mg/kg.
Showed lower tumor burden both on day 23 and 29, compared to the control group.
Molecular Weight

356.42

Formula

C22H20N4O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (350.71 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 2.8057 mL 14.0284 mL 28.0568 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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

×
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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8057 mL 14.0284 mL 28.0568 mL 70.1420 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL 14.0284 mL
10 mM 0.2806 mL 1.4028 mL 2.8057 mL 7.0142 mL
15 mM 0.1870 mL 0.9352 mL 1.8705 mL 4.6761 mL
20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5071 mL
25 mM 0.1122 mL 0.5611 mL 1.1223 mL 2.8057 mL
30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL
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BI-1347 Related Classifications

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.

Keywords:

BI-13472163056-91-3BI1347BI 1347CDKCyclin dependent kinaseoral activityselectivityanti-tumoral activitymouse splenic NK cellhuman NK92MI cellInhibitorinhibitorinhibit

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