MI-3

Modify Date: 2024-01-09 17:18:30

MI-3 Structure
MI-3 structure
Common Name MI-3
CAS Number 1271738-59-0 Molecular Weight 375.555
Density 1.4±0.1 g/cm3 Boiling Point 527.9±60.0 °C at 760 mmHg
Molecular Formula C18H25N5S2 Melting Point N/A
MSDS N/A Flash Point 273.1±32.9 °C

 Use of MI-3


MI-3 is a Menin-MLL interaction inhibitor with IC50 value of 648 ± 25 nM.IC50 value: 648 ± 25 nM [1]Target: Menin-MLLin vitro: The menin-MLL inhibitors very effectively blocked proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM for MI-2 and MI-3. MI-2 and MI-3 showed only a small effect on the cell growth of E2A-HLF transduced BMC (GI50 > 50 μM). MI-2 and MI-3 substantially and specifically reduce the immortalization potential of cells transformed with MLL fusion oncoproteins [1].in vivo: MLL-AF9 transformed BMC that remained viable after 7 days of treatment with MI-2 and MI-3 showed substantial changes in morphology, indicative of monocytic differentiation, as evidenced by increased cell size, lower nuclear to cytoplasmic ratio and highly vacuolated cytoplasm. Consistent with the change in cell morphology, the expression of CD11b was substantially increased on MLL-AF9 transformed BMC after 7 days of treatment with MI-2 and MI-3 [1].

 Names

Name 4-[4-(5,5-dimethyl-4H-thiazol-2-yl)piperazin-1-yl]-2-isopropyl-th ieno[2,3-d]pyrimidine
Synonym More Synonyms

 MI-3 Biological Activity

Description MI-3 is a Menin-MLL interaction inhibitor with IC50 value of 648 ± 25 nM.IC50 value: 648 ± 25 nM [1]Target: Menin-MLLin vitro: The menin-MLL inhibitors very effectively blocked proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM for MI-2 and MI-3. MI-2 and MI-3 showed only a small effect on the cell growth of E2A-HLF transduced BMC (GI50 > 50 μM). MI-2 and MI-3 substantially and specifically reduce the immortalization potential of cells transformed with MLL fusion oncoproteins [1].in vivo: MLL-AF9 transformed BMC that remained viable after 7 days of treatment with MI-2 and MI-3 showed substantial changes in morphology, indicative of monocytic differentiation, as evidenced by increased cell size, lower nuclear to cytoplasmic ratio and highly vacuolated cytoplasm. Consistent with the change in cell morphology, the expression of CD11b was substantially increased on MLL-AF9 transformed BMC after 7 days of treatment with MI-2 and MI-3 [1].
Related Catalog
References

[1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 527.9±60.0 °C at 760 mmHg
Molecular Formula C18H25N5S2
Molecular Weight 375.555
Flash Point 273.1±32.9 °C
Exact Mass 375.155121
PSA 98.16000
LogP 3.23
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.713
Storage condition -20℃
Water Solubility Insuluble (4.5E-3 g/L) (25 ºC)

 Synonyms

Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)-
4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-isopropylthieno[2,3-d]pyrimidine
4-[4-(5,5-Dimethyl-4,5-dihydro-1,3-thiazol-2-yl)-1-piperazinyl]-6-isopropylthieno[2,3-d]pyrimidine
Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-2-(1-methylethyl)-
4-[4-(5,5-Dimethyl-4,5-dihydro-1,3-thiazol-2-yl)-1-piperazinyl]-2-isopropylthieno[2,3-d]pyrimidine
MI-3 (Menin-MLL Inhibitor)
MI-3
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