Art. -Nr.: HY-153244

MFH290

Name: MFH290
Brand: MedChemExpress
SKU: HY-153244
Price: 260.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

MFH290 is an orally active, selective covalent CDK12/CDK13 inhibitor, with an IC₅₀ of 25 nM against human CDK12 and 49 nM against human CDK13. MFH290 reduces the phosphorylation level of CTD-RNAPII-Ser2, downregulates genes related to DNA damage response (DDR), and inhibits transcription factors regulated by super-enhancers. MFH290 can be used in research related to various cancers including leukemia.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.29%
CAS. Nr.: 2088715-91-5
Formel: C₂₆H₃₁N₅O₃S₂
Molecular Weight:525.69

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

MFH290 Chemical Structure

CAS. Nr.: 2088715-91-5

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

HY-103618
THZ531

CDK12/13 Inhibitor

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CDK12

25 nM (IC₅₀)

CDK13

49 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HAP1	IC₅₀	10.15 nM Compound: 1d; MFH290	Antiproliferative activity against human HAP1 cells measured after 72 hrs by Celltiter glo assay Antiproliferative activity against human HAP1 cells measured after 72 hrs by Celltiter glo assay	[PMID: 32502343]
HAP1	IC₅₀	115.7 nM Compound: 1d; MFH290	Antiproliferative activity against human HAP1 cells harboring CDK12 C1039S mutant measured after 72 hrs by Celltiter glo assay Antiproliferative activity against human HAP1 cells harboring CDK12 C1039S mutant measured after 72 hrs by Celltiter glo assay	[PMID: 32502343]
HAP1	IC₅₀	246.5 nM Compound: 1d; MFH290	Antiproliferative activity against human HAP1 cells harboring CDK12 C1039S/CDK13 C1017S double mutant measured after 72 hrs by Celltiter glo assay Antiproliferative activity against human HAP1 cells harboring CDK12 C1039S/CDK13 C1017S double mutant measured after 72 hrs by Celltiter glo assay	[PMID: 32502343]
HAP1	IC₅₀	8.414 nM Compound: 1d; MFH290	Antiproliferative activity against human HAP1 cells harboring CDK13 C1017S mutant measured after 72 hrs by Celltiter glo assay Antiproliferative activity against human HAP1 cells harboring CDK13 C1017S mutant measured after 72 hrs by Celltiter glo assay	[PMID: 32502343]
Sf9	IC₅₀	120 nM Compound: 1d; MFH290	Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA1 expressed in baculovirus infected Sf9 insect cells using FRET-labeled Ser/Thr 12 as substrate measured after 1 hr by Z'-lyte assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA1 expressed in baculovirus infected Sf9 insect cells using FRET-labeled Ser/Thr 12 as substrate measured after 1 hr by Z'-lyte assay	[PMID: 32502343]
Sf9	IC₅₀	3130 nM Compound: 1d; MFH290	Inhibition of kinase tracer 236 binding to recombinant human N-terminal GST-tagged full-length CDK14/Cyclin Y (2 to end residues) expressed in baculovirus infected Sf9 insect cells measured after 1 hr by LanthaScreen Eu Kinase Binding Assay Inhibition of kinase tracer 236 binding to recombinant human N-terminal GST-tagged full-length CDK14/Cyclin Y (2 to end residues) expressed in baculovirus infected Sf9 insect cells measured after 1 hr by LanthaScreen Eu Kinase Binding Assay	[PMID: 32502343]
Sf9	IC₅₀	3830 nM Compound: 1d; MFH290	Inhibition of kinase tracer 236 binding to recombinant human N-terminal GST-tagged human CDK16 (107 to end residues)/Cyclin Y (2 to end residues) expressed in baculovirus infected Sf9 insect cells measured after 1 hr by LanthaScreen Eu Kinase Binding Assa Inhibition of kinase tracer 236 binding to recombinant human N-terminal GST-tagged human CDK16 (107 to end residues)/Cyclin Y (2 to end residues) expressed in baculovirus infected Sf9 insect cells measured after 1 hr by LanthaScreen Eu Kinase Binding Assa	[PMID: 32502343]

In Vitro

MFH290 potently inhibits purified CDK12 (IC₅₀ = 25 nM) and CDK13 (IC₅₀ = 49 nM), exhibits 5-fold selectivity over CDK2 and CDK9, and shows broad selectivity against other human kinases^[1].
MFH290 covalently binds to CDK12/13 in Jurkat T-ALL and HAP1 CML cells^[2].
MFH290 (incubated for 72 h) exhibits nanomolar antiproliferative activity in wild-type HAP1 cells (IC₅₀ = 10.15 nM), while reduced sensitivity is observed in CDK12 C1039S mutant cells and CDK12/CDK13 double mutant cells, indicating that CDK12 is the primary target mediating its antiproliferative effect^[2].
MFH290 (40-200 nM; 6 h) reduces the phosphorylation levels of total Pol II and Pol II CTD at Ser2, Ser5 and Ser7 residues in wild-type HAP1 cells, and this effect is mainly dependent on the inhibition of CDK12^[2].
MFH290 (40-200 nM; 6-24 h) reduces the expression of DDR genes (BRCA2, RAD51, RAD51C) at both RNA and protein levels in wild-type HAP1 cells, and this effect is mainly dependent on the inhibition of CDK12^[2].
MFH290 (1.56-100 nM; 8 days) acts synergistically with the PARP inhibitor Olaparib (HY-10162) to inhibit the proliferation of WT HAP1 cells^[2].

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

Western Blot Analysis^[2]

Cell Line:

WT HAP1 cells, CDK12 C1039S HAP1 cells, CDK13 C1017S HAP1 cells, CDK12 C1039S/CDK13 C1017S double mutant HAP1 cells
Concentration:

40, 200 nM
Incubation Time:

6 h
Result:

Reduced levels of total Pol II and phosphorylated Ser2, Ser5, and Ser7 in WT HAP1 cells.
Greatly restored total and phosphorylated Pol II levels to near WT levels in CDK12 mutant cells.
Showed minimal rescue of total and phosphorylated Pol II levels in CDK13 mutant cells.
Resulted in complete rescue of total and phosphorylated Pol II levels in double mutant cells.

Cell Proliferation Assay^[2]

Cell Line:

WT HAP1 cells
Concentration:

1.56, 6.25, 25, 100 nM MFH290; 44, 133, 400, 1200, 3600 nM Olaparib
Incubation Time:

8 days
Result:

Exhibited synergistic antiproliferative effects with Olaparib, with maximum synergy observed at 25 nM MFH290 and 1.2 μM olaparib, resulting in an excess over Bliss score of 0.75.

Parmacokinetics

Species	Dose	Route	C₀	AUC_last	T_1/2	CL	V_ss	T_max	C_max	F
Mice^[2]	1 mg/kg	i.v.	1312.89 ng/mL	162.22 ng·h/mL	0.17 h	102.03 mL/min/kg	730 mL/kg	/	/	/
Mice^[2]	5 mg/kg	i.p.	/	393.63 ng·h/mL	0.15 h	/	/	0.08 h	885.05 ng/mL	49 %
Mice^[2]	10 mg/kg	p.o.	/	412.44 ng·h/mL	/	/	/	0.25 h	556.46 ng/mL	25 %

In Vivo

MFH290 (1-10 mg/kg; i.v.; i.p.; p.o.) exhibits a short plasma half-life and high clearance in male Swiss albino mice^[2].

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

Chemical Information

CAS. Nr. 2088715-91-5
Appearance Solid
Molecular Weight 525.69
Formel C₂₆H₃₁N₅O₃S₂
Color White to off-white
SMILES

O=C(C1=CC=C(C=C1)NC(C=C)=O)N2C[C@@H](CCC2)NC3=NC=C(SCC4=NC=C(C(C)(C)C)O4)S3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

All

Sort by:

Journal Impact Factor

bioRxiv

Disruption of Microhomology-mediated End-joining in Ewing Sarcoma. [Abstract]

2025 May 10:2025.05.06.651696. PMID: 40568108

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (190.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9023 mL

9.5113 mL

19.0226 mL

5 mM

0.3805 mL

1.9023 mL

3.8045 mL

10 mM

0.1902 mL

0.9511 mL

1.9023 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (4.76 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.76 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tadesse S, et al. The promise and current status of CDK12/13 inhibition for the treatment of cancer. Future medicinal chemistry. 2021 Jan;13(2):117-141. [Content Brief]

[2]. Liu Y, et al. Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. Journal of medicinal chemistry. 2020 Jul 09;63(13):6708-6726. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.9023 mL	9.5113 mL	19.0226 mL	47.5565 mL
	5 mM	0.3805 mL	1.9023 mL	3.8045 mL	9.5113 mL
	10 mM	0.1902 mL	0.9511 mL	1.9023 mL	4.7557 mL
	15 mM	0.1268 mL	0.6341 mL	1.2682 mL	3.1704 mL
	20 mM	0.0951 mL	0.4756 mL	0.9511 mL	2.3778 mL
	25 mM	0.0761 mL	0.3805 mL	0.7609 mL	1.9023 mL
	30 mM	0.0634 mL	0.3170 mL	0.6341 mL	1.5852 mL
	40 mM	0.0476 mL	0.2378 mL	0.4756 mL	1.1889 mL
	50 mM	0.0380 mL	0.1902 mL	0.3805 mL	0.9511 mL
	60 mM	0.0317 mL	0.1585 mL	0.3170 mL	0.7926 mL
	80 mM	0.0238 mL	0.1189 mL	0.2378 mL	0.5945 mL
	100 mM	0.0190 mL	0.0951 mL	0.1902 mL	0.4756 mL

Bioz

Keywords

MFH290

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

MFH290

Publications Citing Use of MedChemExpress (MCE) MFH290

Alle CDK Isoform-spezifische Produkte anzeigen