Romaciclib monohydrochloride
Based on 8 publication(s) in Google Scholar
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
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- Pureté : 99.29%
- CAS No.: 2443816-41-7
- Formule: C15H19Br2ClN4
- Masse moléculaire:450.60
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Romaciclib monohydrochloride
More- Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]
- Blood. 2026 Feb 24:blood.2025031486. [Abstract]
- Nat Commun. 2024 Mar 19;15(1):2198. [Abstract]
- Nat Commun. 2019 Oct 18;10(1):4741. [Abstract]
- Adv Sci (Weinh). 2025 Nov 19:e18346. [Abstract]
- Int J Mol Sci. 2022 Feb 24;23(5):2493. [Abstract]
- bioRxiv. 2025 January 24.
- Friedrich-Alexander-Universität Erlangen-Nürnberg. 2023 Jun 23.
Activité biologique
Description
IC50 & Target
[1]|
CDK8/CycC 4.4 nM (IC50) |
CDK19/CycC 10.4 nM (IC50) |
CDK9/cycT 1070 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | GI50 |
53.9 μM
Compound: SEL120-34A
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Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
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[PMID: 36068975] |
| GES1 | GI50 |
55.3 μM
Compound: SEL120-34A
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Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
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[PMID: 36068975] |
| HCT-116 | GI50 |
11.3 μM
Compound: SEL120-34A
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Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
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[PMID: 36068975] |
| HT-29 | GI50 |
33.8 μM
Compound: SEL120-34A
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Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
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[PMID: 36068975] |
| SW480 | GI50 |
17.7 μM
Compound: SEL120-34A
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Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
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[PMID: 36068975] |
In Vitro
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7[1].
SEL120-34A (1.6 nM-5 μM) inhibits the growth of STAT5 S726 positive KG-1 AML cells, but is not cytotoxic to S726 negative MOLM13 AML cells[1].
SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Chemical Information
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CAS No. 2443816-41-7
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Appearance Solid
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Masse moléculaire 450.60
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Formule C15H19Br2ClN4
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Color White to off-white
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SMILES
CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2.Cl
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Synonyms
SEL120-34A monohydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (8)
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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 -
Blood
Overcoming menin inhibitor resistance in AML cells with combinations including BET proteins and a dual BRG1/BRM inhibitor. [Abstract]2026 Feb 24:blood.2025031486. PMID: 41734382 -
Nat Commun
Oncogenic enhancers prime quiescent metastatic cells to escape NK immune surveillance by eliciting transcriptional memory. [Abstract]2024 Mar 19;15(1):2198. PMID: 38503727 -
Nat Commun
2019 Oct 18;10(1):4741. PMID: 31628323 -
Adv Sci (Weinh)
NUDT21-mediated Alternative Polyadenylation of CDK19 Reprograms Cholesterol Biosynthesis to Drive Colorectal Cancer Progression. [Abstract]2025 Nov 19:e18346. PMID: 41255211 -
Int J Mol Sci
Cyclin-Dependent Kinases (CDKs) and the Human Cytomegalovirus-Encoded CDK Ortholog pUL97 Represent Highly Attractive Targets for Synergistic Drug Combinations. [Abstract]2022 Feb 24;23(5):2493. PMID: 35269635 -
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Solvant et solubilité
In Vitro:
H2O : 50 mg/mL (110.96 mM; Need ultrasonic)
DMSO : 16.67 mg/mL (37.00 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (3.71 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 14.29 mg/mL (31.71 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 2.2193 mL | 11.0963 mL | 22.1926 mL | 55.4816 mL |
| 5 mM | 0.4439 mL | 2.2193 mL | 4.4385 mL | 11.0963 mL | |
| 10 mM | 0.2219 mL | 1.1096 mL | 2.2193 mL | 5.5482 mL | |
| 15 mM | 0.1480 mL | 0.7398 mL | 1.4795 mL | 3.6988 mL | |
| 20 mM | 0.1110 mL | 0.5548 mL | 1.1096 mL | 2.7741 mL | |
| 25 mM | 0.0888 mL | 0.4439 mL | 0.8877 mL | 2.2193 mL | |
| 30 mM | 0.0740 mL | 0.3699 mL | 0.7398 mL | 1.8494 mL | |
| H2O | 40 mM | 0.0555 mL | 0.2774 mL | 0.5548 mL | 1.3870 mL |
| 50 mM | 0.0444 mL | 0.2219 mL | 0.4439 mL | 1.1096 mL | |
| 60 mM | 0.0370 mL | 0.1849 mL | 0.3699 mL | 0.9247 mL | |
| 80 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6935 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2219 mL | 0.5548 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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