ChemicalBook > CAS DataBase List > MI-136

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

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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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 19245
Product name: MI-136
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 19245
Product name: MI-136
Purity: ≥98%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 19245
Product name: MI-136
Purity: ≥98%
Packaging: 10mg
Price: $283
Updated: 2024/03/01

Cayman Chemical

Product number: 19245
Product name: MI-136
Purity: ≥98%
Packaging: 25mg
Price: $618
Updated: 2024/03/01

ChemScene

Product number: CS-5526
Product name: MI-136
Purity: 98.64%
Packaging: 5mg
Price: $105
Updated: 2021/12/16

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MI-136 Chemical Properties,Usage,Production

Description

MI-136 is an inhibitor of the menin-MLL interaction (IC₅₀ = 31 nM; K_d = 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 T_1/2 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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1628316-74-4, MI-136Related Search:

SAR405838 (MI-773) MI-3 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor) CeftazidiMe

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

PPI,MI 136,Apoptosis,inhibit,MI136,Inhibitor,CRPC,castration,cancer,resistant,MI-136,Androgen Receptor,Epigenetic Reader Domain,prostate

5-((4-((6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile

MI-136, 10 mM in DMSO

1628316-74-4

C23H21F3N6S