MI-136
Modify Date: 2024-01-14 18:24:43
MI-136 structure
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Common Name | MI-136 | ||
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| CAS Number | 1628316-74-4 | Molecular Weight | 470.51300 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H21F3N6S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of MI-136MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes. Target: androgen receptorin vitro: MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that were bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage. Furthermore, treatment with MI-136 blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer. [1]in vivo: Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) led to a modest but significant reduction in tumor volume with no effect on mouse body weight. [1] |
| Name | 5-[(4-{[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino}piperidin-1-yl)methyl]-1H-indole-2-carbonitrile |
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| Synonym | More Synonyms |
| Description | MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes. Target: androgen receptorin vitro: MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that were bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage. Furthermore, treatment with MI-136 blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer. [1]in vivo: Treatment of VCaP tumor-bearing mice with MI-136 (40mg/kg) led to a modest but significant reduction in tumor volume with no effect on mouse body weight. [1] |
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| Related Catalog | |
| References |
| Molecular Formula | C23H21F3N6S |
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| Molecular Weight | 470.51300 |
| Exact Mass | 470.15000 |
| PSA | 108.87000 |
| LogP | 5.23648 |
| Storage condition | -20℃ |
| MI-136 |
| 5-[[4-[[6-[2,2,2-tris(fluoranyl)ethyl]thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]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 |