1628316-74-4
5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile
CAS: 1628316-74-4
Molecular Formula: C23H21F3N6S
1628316-74-4 - Names and Identifiers
1628316-74-4 - Physico-chemical Properties
| Molecular Formula | C23H21F3N6S |
| Molar Mass | 470.51 |
| Density | 1.45±0.1 g/cm3(Predicted) |
| Boling Point | 654.9±55.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| pKa | 14.20±0.30(Predicted) |
| Storage Condition | -20℃ |
| Use | MI-136 is an inhibitor of menin-MLL (PPI) protein interaction with an IC50 value of 31 nM and a Kd value of 23.6 nM. MI-136 can inhibit AR signaling pathway and has the potential to be used in castration-resistant tumors. |
| Target | Androgen Receptor |
| In vitro study | AR positive cell lines such as VCaP, LNCaP and 22RV1 are MI-136 sensitive, and MI-136 treatment can inhibit the expression of genes binding to ASH2L and induce apoptosis of VCaP cells after AR stimulation, DHT-induced cell proliferation was prevented in AR-dependent cell lines (LNCaP and VCaP). MI-136 has an effect on cell proliferation similar to that of MDV-310 (a second-generation FDA-approved antiandrogen for the treatment of refractory prostate cancer) |
| In vivo study | Mice bearing VCaP tumors were administered MI-136(40mg/kg), and the tumor volume was significantly reduced, but there was no effect on the body weight of the mice. |
1628316-74-4 - Reference
| Reference Show more | 1. Dmitry Borkin, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.2. Rohit Malik, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52. |
1628316-74-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.125 ml | 10.627 ml | 21.253 ml |
| 5 mM | 0.425 ml | 2.125 ml | 4.251 ml |
| 10 mM | 0.213 ml | 1.063 ml | 2.125 ml |
| 5 mM | 0.043 ml | 0.213 ml | 0.425 ml |
Last Update：2024-01-02 23:10:35
1628316-74-4 - Cell Experiment
To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM MI-136 for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and MI-136 for 48 hrs. Cells are then stimulated with 10nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays. (Only for Reference) Cell lines: VCaP cells
Last Update：2023-08-16 21:32:38
1628316-74-4 - Reference Information
| biological activity | MI-136 inhibit the expression of androgen receptor (AR) targeting genes induced by DHT. |
| target | TargetValue Menin-MLL interaction () |
| Target | Value |
| in vitro study | AR-positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. MI-136 treatment will inhibit the expression of genes bound to ASH2L after AR stimulation, induce apoptosis of VCaP cells, and prevent DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to that of MDV-310 (a second-generation FDA-certified antiandrogen drug for the treatment of refractory prostate cancer) |
| in vivo study | MI-136(40 mg/kg) was applied to mice carrying VCaP tumor, and the tumor volume was significantly reduced, but it had no effect on the weight of mice. |
Last Update：2024-04-09 02:00:01
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