MI-136

SKU: orb1226024

Description

A potent Menin-MLL interaction inhibitor with IC50 of 31 nM; demonstrates potent inhibitory activity and strong binding affinity to menin.

Key Properties

• CAS Number: 1628316-74-4
• MW: 470.5132
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₁F₃N₆S
• SMILES: C1CN(CCC1NC2=C3C=C(SC3=NC=N2)CC(F)(F)F)CC4=CC5=C(C=C4)NC(=C5)C#N
• Target: HMTase
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• In Vivo:
  MI-136 exhibits T1/2 of 3.1 h after po administration. MI-136 (40 mg/kg, ip) leads to a significant decrease in the growth of castration-resistant VCaP tumors. Animal model: VCaP xenografts. 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.
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• In Vitro:
  MI-136 (0-20) exhibits IC50values of 5.59 μM, 7.15 μM, 5.37 μM and 19.76 μM in LNCaP, VCaP, 22rv1 and PNT2 cells. Cell Proliferation Assay Cell line: AR positive cell lines such as VCaP, LNCaP and 22RV1. Concentration: 0-20 μM. Incubation time: 24 h. Result: Inhibited cell proliferation.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MI 136 | MI136

Quick Database Links

Gene Symbol

HMTase