MI-136
- Product Name
- MI-136
- CAS No.
- 1628316-74-4
- Chemical Name
- MI-136
- Synonyms
- MI-136;CS-2162;MI136;MI 136;HY-19319 (MI 136;MI-136, 10 mM in DMSO;MI-136;HY-19319 (MI 136; MI136);;5-((4-((6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-in;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-indole-2-carbonitrile;1H-Indole-2-carbonitrile, 5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-
- CBNumber
- CB83121119
- Molecular Formula
- C23H21F3N6S
- Formula Weight
- 470.51
- MOL File
- 1628316-74-4.mol
MI-136 Property
- 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
N-Bromosuccinimide Price
- Product number
- 19245
- Product name
- MI-136
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 19245
- Product name
- MI-136
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 19245
- Product name
- MI-136
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 19245
- Product name
- MI-136
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $618
- Updated
- 2024/03/01
- Product number
- CS-5526
- Product name
- MI-136
- Purity
- 98.64%
- Packaging
- 5mg
- Price
- $105
- Updated
- 2021/12/16
MI-136 Chemical Properties,Usage,Production
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-136 Preparation Products And Raw materials
Raw materials
Preparation Products
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