Product Name :
M-1211
Description:
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.
CAS:
2377337-93-2
Molecular Weight:
793.00
Formula:
C42H57FN6O6S
Chemical Name:
methyl N-[(1S, 2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-(1-[3-methoxy-1-(4-[(1S, 4S)-5-(prop-2-enoyl)-2, 5-diazabicyclo[2.2.1]heptan-2-yl]sulfonylphenyl)azetidin-3-yl]methylpiperidin-4-yl)ethyl]cyclopentyl]carbamate
Smiles :
COC(=O)N[C@H]1CCC[C@@H]1[C@@](CN1CCC1)(C1CCN(CC2(CN(C2)C2=CC=C(C=C2)S(=O)(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C=C)OC)CC1)C1=CC(F)=CC=C1
InChiKey:
HFHVSSGMYSWPIR-SZDLQPMWSA-N
InChi :
InChI=1S/C42H57FN6O6S/c1-4-39(50)48-24-35-23-34(48)25-49(35)56(52,53)36-14-12-33(13-15-36)47-27-41(28-47,55-3)26-46-20-16-30(17-21-46)42(29-45-18-7-19-45,31-8-5-9-32(43)22-31)37-10-6-11-38(37)44-40(51)54-2/h4-5,8-9,12-15,22,30,34-35,37-38H,1,6-7,10-11,16-21,23-29H2,2-3H3,(H,44,51)/t34-,35-,37-,38-,42-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.|Product information|CAS Number: 2377337-93-2|Molecular Weight: 793.00|Formula: C42H57FN6O6S|Chemical Name: methyl N-[(1S, 2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-(1-[3-methoxy-1-(4-[(1S, 4S)-5-(prop-2-enoyl)-2, 5-diazabicyclo[2.2.1]heptan-2-yl]sulfonylphenyl)azetidin-3-yl]methylpiperidin-4-yl)ethyl]cyclopentyl]carbamate|Smiles: COC(=O)N[C@H]1CCC[C@@H]1[C@@](CN1CCC1)(C1CCN(CC2(CN(C2)C2=CC=C(C=C2)S(=O)(=O)N2C[C@@H]3C[C@H]2CN3C(=O)C=C)OC)CC1)C1=CC(F)=CC=C1|InChiKey: HFHVSSGMYSWPIR-SZDLQPMWSA-N|InChi: InChI=1S/C42H57FN6O6S/c1-4-39(50)48-24-35-23-34(48)25-49(35)56(52,53)36-14-12-33(13-15-36)47-27-41(28-47,55-3)26-46-20-16-30(17-21-46)42(29-45-18-7-19-45,31-8-5-9-32(43)22-31)37-10-6-11-38(37)44-40(51)54-2/h4-5,8-9,12-15,22,30,34-35,37-38H,1,6-7,10-11,16-21,23-29H2,2-3H3,(H,44,51)/t34-,35-,37-,38-,42-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Emodin Description |Shelf Life: ≥12 months if stored properly.Clomipramine Description |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:33164621 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|M-1121 (0~100 nM; 24 hours; MV4;11 cells) drives dose-dependent down-regulation of HOXA9 and MEIS1 gene expression in the MLL-rearranged MV4;11 leukemia cell line. M-1121 establishes covalent interactions with Cysteine 329 located in the MLL binding pocket of menin and potently inhibits growth of acute leukemia cell lines carrying MLL translocations with no activity in cell lines with wild-type MLL.|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%. 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. M-1121 (5 mg/kg; p.o.) has a low clearance and a moderate volume of distribution.|Products are for research use only. Not for human use.|
