| Identification | Back Directory | [Name]
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid | [CAS]
1072833-77-2 | [Synonyms]
MLN2238
CS-1976
IxazoMib
Ixazomib-d7
ixazomib(MLN2238)
MLN2238(iaxzomib)
MLN2238(Ixazomib)
Ixazomib (MLN-9708)
Ixazomib (10mM in DMSO)
MLN2238;MLN 2238;MLN-2238
IXAZOMIB;MLN 2238;MLN-2238
1-(2-(2,5-dichlorobenzamido)acetamido)-
3-methylbutylboronic acid
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid
(R)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbuyl)boronic acid
(1R)-1-{2-[(2,5-dichlorophenyl)formamido]acetamido}-3-methylbutyl]boronic acid
B-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid
Boronic acid, B-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-
Ixazomib-13C2,15NQ: What is
Ixazomib-13C2,15N Q: What is the CAS Number of
Ixazomib-13C2,15N
B-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid Ixazomib (MLN2238)
Ixazomib, 98%, a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM) | [EINECS(EC#)]
810-246-8 | [Molecular Formula]
C14H19BCl2N2O4 | [MDL Number]
MFCD18251438 | [MOL File]
1072833-77-2.mol | [Molecular Weight]
361 |
| Chemical Properties | Back Directory | [Melting point ]
>142°C (subl.) | [density ]
1.306 | [storage temp. ]
-20°C Freezer | [solubility ]
DMSO (Sparingly), Methanol (Slightly) | [form ]
Solid | [pka]
9.67±0.43(Predicted) | [color ]
White to Pale Yellow |
| Hazard Information | Back Directory | [Uses]
Ixazomib is a proteasome inhibitor that acts by preventing cell growth in solid tumours. It is an anticancer agent that is used to treat patients with multiple myeloma and is potentially neurotoxic. | [Definition]
ChEBI: A glycine derivative that is the amide obtained by formal condensation of the carboxy group of N-(2,5-dichlorobenzoyl)glycine with the amino group of [(1R)-1-amino-3-methylbutyl]boronic acid. The active metabolite of ixa
omib citrate, it is used in combination therapy for treatment of multiple myeloma. | [Synthesis]
The diol borate ester (5 g) of MLN9708 intermediate was mixed with concentrated hydrochloric acid (5 mL), boric acid (1.9 g) and diisopropyl ether (100 mL) at room temperature. After the reaction mixture was stirred for 5 hours, the solid product was collected by filtration and washed with diisopropyl ether (25 mL). Subsequently, the resulting solid was dried under vacuum conditions to give the final (R)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic acid (Txazomib) in 86.5% yield. | [in vivo]
Ixazomib (MLN2238) shows antitumor activity in the CWR22 xenograft model. The antitumor effects of Ixazomib (MLN2238) dosed at 14 mg/kg i.v. or 7 mg/kg i.v. are compared with Bortezomib dosed at 0.8 mg/kg i.v. or 0.4 mg/kg i.v. on a twice weekly regimen. The high dose for both Ixazomib (MLN2238) and Bortezomib (HY-10227) shows similar antitumor activity in this model (T/C=0.36 and 0.44, respectively). However, Ixazomib (MLN2238) (7 mg/kg) shows greater efficacy at a 0.5 MTD dose compared with a 0.5 MTD dose of Bortezomib (0.4 mg/kg; T/C=0.49 compared with T/C=0.79, respectively) Ixazomib (MLN2238) shows time-dependent reversible proteasome inhibition; however, the proteasome dissociation half-life (t1/2) for Ixazomib (MLN2238) is determined to be 18 minutes[1]. | [target]
chymotrypsin-like proteolytic (β5) site of the 20S proteasome | [References]
[1] Patent: WO2018/158697, 2018, A1. Location in patent: Page/Page column 25 |
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