BI-1347
Based on 7 publication(s) in Google Scholar
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.
The BI-1347 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Purity: 99.85%
- CAS No.: 2163056-91-3
- Formula: C22H20N4O
- Molecular Weight:356.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BI-1347
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
Biological Activity
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CDK8 1.1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
32.94 μM
Compound: BI-1347
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
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[PMID: 36930701] |
| HEK293 | EC50 |
5 nM
Compound: 28; BI-1347
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Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence as
Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence as
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[PMID: 32071678] |
| MDA-MB-231 | IC50 |
28.65 μM
Compound: BI-1347
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
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[PMID: 36930701] |
| MDA-MB-468 | IC50 |
28.82 μM
Compound: BI-1347
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 4 days by Celltiter glo luminescent assay
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[PMID: 36930701] |
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.
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Cell Line:Mouse splenic NK cells
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Concentration:150 nM
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Incubation Time:44 hours
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Result:Increased the proportion of granzyme B-positive NK cells by approximately 4-fold.
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Cell Line:Human NK92MI cells
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Concentration:0.1 nM-10 μM
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Incubation Time:24 hours
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Result:Increased perforin levels with an EC50 value of 7.2 nM.
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.
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Animal Model:B16-F10-luc2 syngeneic melanoma model[2]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg; once daily; 30 d
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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.
Chemical Information
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CAS No. 2163056-91-3
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Appearance Solid
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Molecular Weight 356.42
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Formula C22H20N4O
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Color Light yellow to yellow
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SMILES
O=C(N(C)C)CN1N=CC(C2=CC=C(C3=CN=CC4=C3C=CC=C4)C=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell
2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809 -
Oncogenesis
2026 Apr 24;15(1):27. PMID: 42031714 -
Pharmaceuticals (Basel)
New Assay Systems to Characterize the Broad-Spectrum Antiherpesviral and Non-Herpesviral Activity of Cyclin-Dependent Kinase (CDK) 8 Inhibitors. [Abstract]2025 Oct 16;18(10):1560. PMID: 41155676
BI-1347 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]
CDK8 inhibitor (BI-1347 (0.0001-100 μM; 4 days) were assessed for their level of cytotoxicity by a Neutral Red uptake assay (orange) and their antiviral activity (black) on COS-7 cells.
BI-1347 purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]
Summarized results for different cell types (Vero, COS-7 and HFFs) or different method approaches (GFP or qPCR) for the CDK8 inhibitors (BI-1347, CCT-251921, MSC-2530818) or reference compounds (BCV, CDV, GCV) based on the EC50, CC50, and SI of at least three replications; n.d. not determined.
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BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.
MCF10A cells were plated at equal low density and either mock treated or treated with 31 nM BI-1347, in the presence or absence of 1.25 µM or 10 µM XL413 over a 7-day period. Representative image of plates stained with crystal violet. The results showed that adding the CDK8 inhibitor BI-1347 to MCF10A cells only marginally inhibited their proliferation; in contrast, BI-1347 strongly reduced cell growth when BI-1347 was combined with either 1.25 µM or 10 µM of the CDC7i XL413.
BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.
MCF10A cells were mock treated or treated for 24 hours with three different CDK8 inhibitors: 31 nM BI-1347, 5 µM Senexin A, or 100 nM CCT-251921, alone or in combination with either 10 µM XL413 or 0.3 µM TAK-931 CDC7 inhibitors. Cells were labelled with EdU for last 30 minutes and DNA synthesis, DNA content and cell cycle distribution were assessed by flow cytometry.
BI-1347 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 9.
MCF10A cells were either mock treated, treated with 31 nM BI-1347 alone, with 10 µM XL413 with or in combination of both or with 2mM Hydroxyurea (HU) for 24 hours. Whole cell extracts, or soluble and chromatin-enriched fractions were analysed by immunoblotting for the indicated proteins. TPS (total protein stain) is used as a loading control. Asterisks indicate non-specific bands.
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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 |
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| 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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