MI-136
MI-136 Basic information
- Product Name:
- MI-136
- Synonyms:
-
- MI-136
- MI-136;HY-19319 (MI 136; MI136);
- HY-19319 (MI 136
- 1H-Indole-2-carbonitrile, 5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-
- MI136;MI 136
- CS-2162
- 5-[[4-[[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-1H-indole-2-carbonitrile
- 5-((4-((6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-in
- CAS:
- 1628316-74-4
- MF:
- C23H21F3N6S
- MW:
- 470.51
- Mol File:
- 1628316-74-4.mol
MI-136 Chemical Properties
- Boiling point:
- 654.9±55.0 °C(Predicted)
- Density
- 1.45±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 1 mg/ml; DMSO: 1 mg/ml; Ethanol: 10 mg/ml
- form
- A crystalline solid
- pka
- 14.20±0.30(Predicted)
- color
- White to off-white
MI-136 Usage And Synthesis
Description
MI-136 is an inhibitor of the menin-MLL interaction (IC50 = 31 nM; Kd = 23.6 nM). By blocking MLL recruitment predominantly at the level of the menin-MLL interaction, it can inhibit androgen receptor (AR)-mediated transcription. At 40 mg/kg, MI-136 has been shown to block AR signaling, inhibiting the growth of castration-resistant tumors in mice.
Uses
MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors[1][2].
in vivo
MI-136 exhibits T1/2 of 3.1 h after po administration[1].
MI-136 (40 mg/kg, ip) leads to a significant decrease in the growth of castration-resistant VCaP tumors[2].
| Animal Model: | VCaP xenografts[2]. |
| Dosage: | 40 mg/kg. |
| Administration: | Intraperitoneal injection, 5 days a week. |
| Result: | Led to a significant decrease in the growth of castration-resistant VCaP tumors compared to vehicle controls. |
References
[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. DOI:10.1021/acs.jmedchem.5b01305
[2] Rohit Malik, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52. DOI:10.1038/nm.3830
MI-136Supplier
- Tel
- sales@boylechem.com
- Tel
- 021-58955995
- sales@medchemexpress.cn
- Tel
- 0371-55932928 18937192232
- 1282296214@qq.com
- Tel
- 0571-82693216
- info@yuhaochemical.com
- Tel
- 021-52996696，15000506266 15000506266