(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid
- Product Name
- (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid
- CAS No.
- 1072833-77-2
- Chemical Name
- (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid
- Synonyms
- IxazoMib;MLN2238;Ixazomib-d7;CS-1976;Aishazomi;MLN2238(Ixazomib);MLN2238(iaxzomib);ixazomib(MLN2238);Ixazomib (MLN-9708);Ixazomib (10mM in DMSO)
- CBNumber
- CB62521080
- Molecular Formula
- C14H19BCl2N2O4
- Formula Weight
- 361.03
- MOL File
- 1072833-77-2.mol
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid Property
- Melting point:
- >142°C (subl.)
- Density
- 1.306
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Sparingly), Methanol (Slightly)
- pka
- 9.67±0.43(Predicted)
- form
- Solid
- color
- White to Pale Yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H360May damage fertility or the unborn child
H362May cause harm to breast-fed children
- Precautionary statements
-
P201Obtain special instructions before use.
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P263Avoid contact during pregnancy/while nursing.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P308+P313IF exposed or concerned: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- 18385
- Product name
- MLN2238
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 18385
- Product name
- MLN2238
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $193
- Updated
- 2024/03/01
- Product number
- 18385
- Product name
- MLN2238
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $341
- Updated
- 2024/03/01
- Product number
- 18385
- Product name
- MLN2238
- Purity
- ≥95%
- Packaging
- 50mg
- Price
- $1169
- Updated
- 2024/03/01
- Product number
- I942000
- Product name
- Ixazomib
- Packaging
- 100mg
- Price
- $700
- Updated
- 2021/12/16
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid Chemical Properties,Usage,Production
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
1201903-02-7
11113-50-1
1072833-77-2
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
(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid Preparation Products And Raw materials
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View Lastest Price from (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid manufacturers
- Product
- (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid 1072833-77-2
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98%-102%
- Supply Ability
- 100G
- Release date
- 2021-06-29
- Product
- (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid 1072833-77-2
- Price
- US $6.00-1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- g-kg-tons, free sample is available
- Release date
- 2024-03-28
- Product
- (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid 1072833-77-2
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24