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MedKoo Cat#: 462462 | Name: MI-136
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.

Chemical Structure

MI-136
MI-136
CAS#1628316-74-4

Theoretical Analysis

MedKoo Cat#: 462462

Name: MI-136

CAS#: 1628316-74-4

Chemical Formula: C23H21F3N6S

Exact Mass: 470.1500

Molecular Weight: 470.52

Elemental Analysis: C, 58.71; H, 4.50; F, 12.11; N, 17.86; S, 6.81

Price and Availability

Size Price Availability Quantity
5mg USD 305.00 2 Weeks
10mg USD 550.00 2 Weeks
25mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
MI-136; MI136; MI 136
IUPAC/Chemical Name
5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile
InChi Key
PSOJDGBGVBEYJX-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H21F3N6S/c24-23(25,26)10-18-9-19-21(28-13-29-22(19)33-18)31-16-3-5-32(6-4-16)12-14-1-2-20-15(7-14)8-17(11-27)30-20/h1-2,7-9,13,16,30H,3-6,10,12H2,(H,28,29,31)
SMILES Code
FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4)CC3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
The therapeutic capacity of MI-136 was further validated in tumor organoids in vitro and an orthotopic model in vivo. CRISPR/cas9-mediated mutations of major components of the menin-MLL complex, Men1, Kmt2a and Ash2l, inhibited the growth of tumor organoids, suggesting that the complex was the target of MI-136. Transcriptome analysis showed that the hypoxia-inducible factor (HIF) pathway was the most significantly downregulated pathway by MI-136 treatment. Consistently, Men1, Kmt2a, and Ash2l knockout also repressed the expressions of the HIF target genes. Loss of Hif1a or Hif1b partially phenocopied the inhibition of the menin-MLL complex by MI-136 or mutations in term of tumor organoid growth. Further, this study found that MEN1 was upregulated in human endometrial cancers, which were tightly correlated with the expression levels of HIF1A, and associated with poor prognosis. Importantly, MI-136 also significantly inhibited the growth of endometrial cancer organoids derived from patients. Reference: Cancer Gene Ther. 2021 Feb;28(1-2):112-125. https://pubmed.ncbi.nlm.nih.gov/32632269/
In vivo activity:
The therapeutic capacity of MI-136 was further validated in tumor organoids in vitro and an orthotopic model in vivo. CRISPR/cas9-mediated mutations of major components of the menin-MLL complex, Men1, Kmt2a and Ash2l, inhibited the growth of tumor organoids, suggesting that the complex was the target of MI-136. Transcriptome analysis showed that the hypoxia-inducible factor (HIF) pathway was the most significantly downregulated pathway by MI-136 treatment. Consistently, Men1, Kmt2a, and Ash2l knockout also repressed the expressions of the HIF target genes. Loss of Hif1a or Hif1b partially phenocopied the inhibition of the menin-MLL complex by MI-136 or mutations in term of tumor organoid growth. Further, this study found that MEN1 was upregulated in human endometrial cancers, which were tightly correlated with the expression levels of HIF1A, and associated with poor prognosis. Importantly, MI-136 also significantly inhibited the growth of endometrial cancer organoids derived from patients. Reference: Cancer Gene Ther. 2021 Feb;28(1-2):112-125. https://pubmed.ncbi.nlm.nih.gov/32632269/
Solvent mg/mL mM comments
Solubility
DMSO 68.3 145.23
Ethanol 52.0 110.52
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 470.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
Chen J, Zhao L, Peng H, Dai S, Quan Y, Wang M, Wang J, Bi Z, Zheng Y, Zhou S, Liu Y, Chen C, Na F. An organoid-based drug screening identified a menin-MLL inhibitor for endometrial cancer through regulating the HIF pathway. Cancer Gene Ther. 2021 Feb;28(1-2):112-125. doi: 10.1038/s41417-020-0190-y. Epub 2020 Jul 7. PMID: 32632269.
In vitro protocol:
Chen J, Zhao L, Peng H, Dai S, Quan Y, Wang M, Wang J, Bi Z, Zheng Y, Zhou S, Liu Y, Chen C, Na F. An organoid-based drug screening identified a menin-MLL inhibitor for endometrial cancer through regulating the HIF pathway. Cancer Gene Ther. 2021 Feb;28(1-2):112-125. doi: 10.1038/s41417-020-0190-y. Epub 2020 Jul 7. PMID: 32632269.
In vivo protocol:
Chen J, Zhao L, Peng H, Dai S, Quan Y, Wang M, Wang J, Bi Z, Zheng Y, Zhou S, Liu Y, Chen C, Na F. An organoid-based drug screening identified a menin-MLL inhibitor for endometrial cancer through regulating the HIF pathway. Cancer Gene Ther. 2021 Feb;28(1-2):112-125. doi: 10.1038/s41417-020-0190-y. Epub 2020 Jul 7. PMID: 32632269.
1: Malik R, Khan AP, Asangani IA, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015;21(4):344-352. doi:10.1038/nm.3830

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