4H-Imidazo[4,5,1-ij]quinoline, 7,8-dibromo-5,6-dihydro-9-methyl-2-(1-piperazinyl)-
SEL120-34A
CAS: 1609522-33-9
Molecular Formula: C15H18Br2N4
4H-Imidazo[4,5,1-ij]quinoline, 7,8-dibromo-5,6-dihydro-9-methyl-2-(1-piperazinyl)- - Names and Identifiers
| Name | SEL120-34A |
| Synonyms | SEL120 SEL120-34A 1609522-33-9 4H-Imidazo[4,5,1-ij]quinoline, 7,8-dibromo-5,6-dihydro-9-methyl-2-(1-piperazinyl)- |
| CAS | 1609522-33-9 |
4H-Imidazo[4,5,1-ij]quinoline, 7,8-dibromo-5,6-dihydro-9-methyl-2-(1-piperazinyl)- - Physico-chemical Properties
| Molecular Formula | C15H18Br2N4 |
| Molar Mass | 414.14 |
| Density | 1.92±0.1 g/cm3(Predicted) |
| Boling Point | 557.6±60.0 °C(Predicted) |
| pKa | 8.60±0.10(Predicted) |
| In vitro study | SEL120-34A inhibited the kinase activity of CDK8/CyclinC and CDK19/CyclinC with IC50 of 4.4 nM and 10.4 nM, respectively. In Vitro, it does not significantly inhibit other members of the CDK family, such as CDK1/2/4/6/5/7; Whereas SEL120-34A has an IC50 value of 1070 nM for cdk9. In cancer cells, SEL120-34A can inhibit the phosphorylation of STAT1 S727 and STAT5 S726, inhibit the expression of mitogen-induced immediate early response genes, and inhibit IFN response genes. SEL120-34A has strong activity in hematological malignancies, especially in some specific acute myeloid leukemia, acute lymphoblastic leukemia and mantle cell lymphoma. SEL120 − 34A alters the transcriptional program of leukemic cell differentiation-related genes. |
| In vivo study | SEL120-34A has good pharmacodynamics and can affect the expression of CDK8 and CDK19 related genes in vivo. SEL120-34A treatment can cause specific changes in interferon-responsive genes in vivo, inhibiting the proliferation of the AML cell line. SEL120-34A does not affect the normal hematopoietic function. In models inoculated subcutaneously with AML and MCL cells, oral administration of SEL120 − 34A was effective in inhibiting tumor growth. |
4H-Imidazo[4,5,1-ij]quinoline, 7,8-dibromo-5,6-dihydro-9-methyl-2-(1-piperazinyl)- - References
| biological activity | SEL120 (SEL120-34,SEL120-34A) is a novel CDK8 inhibitor, the IC50 values for CDK8 and CDK19 were 4.4 nM and 10.4 nM, respectively. |
| Target | Value |
| CDK8 (Cell-free assay) | 4.4 nM |
| CDK19 (Cell-free assay) | 10.4 nM |
Last Update：2024-04-09 02:00:15
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