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| | Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester Basic information |
| Product Name: | Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester | | Synonyms: | M-1211;M-1121;Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester | | CAS: | 2377337-93-2 | | MF: | C42H57FN6O6S | | MW: | 793 | | EINECS: | | | Product Categories: | | | Mol File: | 2377337-93-2.mol | ![Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester Structure](CAS/20211123/GIF/2377337-93-2.gif) |
| | Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester Chemical Properties |
| density | 1.34±0.1 g/cm3(Predicted) | | pka | 12.12±0.40(Predicted) | | form | Solid | | color | White to yellow |
| | Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester Usage And Synthesis |
| Uses | M1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression[1]. | | in vivo | M-1121 (100 mg/kg; p.o.; 26 days) reduces the average tumor volume from 157 mm3 at the beginning of the treatment to 106 mm3 on day 26 of the treatment, a reduction of tumor volume of 32%[1].
M-1121 (300 mg/kg; p.o.) leads to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment[1].
M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution[1]. | Animal Model: | SCID mice[1] | | Dosage: | 100 mg/kg | | Administration: | P.o. | | Result: | Reduced the average tumor volume from 157 mm3 at the beginning of the treatment to 106 mm3 on day 26 of the treatment, a reduction of tumor volume of 32%.
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| Animal Model: | SCID mice[1] | | Dosage: | 300 mg/kg | | Administration: | P.o. | | Result: | Led to complete tumor regression in 10 out of 10 mice with no tumor regrowth detected up to a month after last treatment.
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| Animal Model: | Female C57BL/6 mice[1] | | Dosage: | 5 mg/kg (Pharmacokinetic Analysis) | | Administration: | P.o. | | Result: | Had a low clearance and a moderate volume of distribution.
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| | References | [1] Zhang M, et al. Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression. J Med Chem. 2021;64(14):10333-10349. DOI:10.1021/acs.jmedchem.1c00789 |
| | Carbamic acid, N-[(1S,2R)-2-[(1S)-2-(1-azetidinyl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-(1-oxo-2-propen-1-yl)-2,5-diazabicyclo[2.2.1]hept-2-yl]sulfonyl]phenyl]-3-azetidinyl]methyl]-4-piperidinyl]ethyl]cyclopentyl]-, methyl ester Preparation Products And Raw materials |
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