2088715-91-5
Chemical Structure
MFH290
- CAS No.: 2088715-91-5
- Formula:C26H31N5O3S2
- Molecular Weight:525.69
IUPAC Name: (R)-N-(4-(3-((5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)amino)piperidine-1-carbonyl)phenyl)acrylamide
InChIKey: COGUZYALRYMQTD-LJQANCHMSA-N
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
Biological Activity: 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[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MFH290 | 98.29% | 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. | ||||||||||||||||||||
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References
- [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]
