MI-136( MI 136 | MI136 )

Catalog No. M12427 CAS No. 1628316-74-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

MI-136
Note

Research use only, not for human use.
Brief Description

A potent Menin-MLL interaction inhibitor with IC50 of 31 nM.
Description

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

MI 136 | MI136
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

AndrogenReceptor
Research Area

Cancer
Indication

——

CAS Number

1628316-74-4
Formula Weight

470.5132
Molecular Formula

C23H21F3N6S
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 31 mg/mL
SMILES

C1CN(CCC1NC2=C3C=C(SC3=NC=N2)CC(F)(F)F)CC4=CC5=C(C=C4)NC(=C5)C#N
Chemical Name

1H-Indole-2-carbonitrile, 5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-

1. Borkin D, et al. J Med Chem. 2016 Feb 11;59(3):892-913. 2. Borkin D, et al. Cancer Cell. 2015 Apr 13;27(4):589-602.

Calculator

molnova catalog