Cas No.: | 1628316-74-4 |
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 |
Synonyms: | MI-136;MI 136;5-((4-((6-(2,2,2-trifluoroethyl)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;PSOJDGBGVBEYJX-UHFFFAOYSA-N;BCP20862;BDBM50156121;s7815;MI 136; MI136;AK475093;Q27454240;5((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl;5-[[4-[[6-(2,2,2-Trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]-1H-indole-2 |
SMILES: | S1C(C([H])([H])C(F)(F)F)=C([H])C2C1=NC([H])=NC=2N([H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C3=C(C([H])=C(C#N)N3[H])C=2[H])C([H])([H])C1([H])[H] |
Formula: | C23N6F3SH21 |
M.Wt: | 470.5132 |
Purity: | 99% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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] |
References: | 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] |