(R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid NEW
| Price | $6 | $5 | $1 |
| Package | 1KG | 25KG | 100KG |
| Min. Order: | 1KG |
| Supply Ability: | g-kg-tons, free sample is available |
| Update Time: | 2024-03-29 |
Product Details
| Product Name: (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid | CAS No.: 1072833-77-2 |
| Min. Order: 1KG | Purity: 99% |
| Supply Ability: g-kg-tons, free sample is available | Release date: 2024/03/29 |
| Lead time: In stock | Packaging: bottle/drum/bucket/IBC, as request. |
| Delivery: By sea, by air, by express | Origin: Manufacturer |
| Name: Sun |
1. Product information
| Name | [(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid |
|---|---|
| Synonym | More Synonyms |
| Description | Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM). |
|---|---|
| Related Catalog | Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome Research Areas >> Cancer |
| Target | IC50: 3.4 nM (20S proteasome)[1] Ki: 0.93 nM (20S proteasome)[1] |
| In Vitro | Ixazomib (MLN2238) is an N-capped dipeptidyl leucine boronic acid and preferentially bound to and inhibited the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nM (Ki of 0.93 nM). At higher concentrations, Ixazomib (MLN2238) also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50 of 31 and 3,500 nM, respectively). Cell viability studies are performed in a variety of mammalian cell lines to compare the in vitro antiproliferative effects of Ixazomib (MLN2238) with Bortezomib. Studies performed with A375 (lung), H460 (lung), HCT-116 (colon), and HT-29 (colon) cells revealed similar LD50 values for the two compounds, which range from 4 to 58 nM[1]. |
| 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 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]. |
| Cell Assay | Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 d before the start of the experiment at 10,000 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or Ixazomib in DMSO (0.5% final, v/v) for 1 h at 37°C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or Ixazomib (MLN2238) for 30 min at 37°C and then washed thrice in medium to remove the compounds. Cells are incubated for an additional 4 h at 37°C, after which the medium is removed and replaced with fresh medium. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents. Luminescence is measured using a LEADseeker instrument[1]. |
| Animal Admin | Mice[1] Male CB17-SCID mice, approximately 8 to 11 wk of age, are inoculated s.c. with freshly dissected CWR22 tumor fragments (~20 mg) in the right dorsal flank. Mean tumor volume (MTV) is calculated using the following formula: 0.5×(length×width2). When MTV reaches approximately 150 to 200 mm3, animals are randomized into treatment groups (n=10 per group) before dosing. Antitumor activity is determined at the end of the study by calculating the treatment over control (T/C) ratio of their MTVs at the end of the study. Rats[1] To determine the pharmacokinetic profile of Ixazomib and Bortezomib in a second species, Sprague-Dawley rats are administered a single i.v. dose of Ixazomib (MLN2238) at either 0.3 or 0.2 mg/kg or Bortezomib at 0.2 mg/kg. Both Ixazomib doses provided a greater plasma exposure (AUC0-48h of 704 and 1,070 h?ng/mL for 0.2 and 0.3 mg/kg doses, respectively) compared with Bortezomib (AUC0-48h of 206 h?ng/mL), confirming that Ixazomib (MLN2238) also has improved plasma exposure compared with Bortezomib in rodents. |
| References | [1]. Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010 Mar 1;70(5):1970-80. |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C14H19BCl2N2O4 |
| Molecular Weight | 361.029 |
| Exact Mass | 360.081482 |
| PSA | 105.64000 |
| LogP | 2.82 |
| Index of Refraction | 1.546 |
| Storage condition | 2-8°C |
| B-{(1R)-1-[2-(2,5-dichlorobenzamido)acetamido]-3-methylbutyl}boronic acid |
| N-(2,5-Dichlorobenzoyl)-N-[(1R)-1-(dihydroxyboryl)-3-methylbutyl]glycinamide |
| [(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methyl-butyl]boronic acid |
| MLN2238 |
| ixazomib |
| Boronic acid, B-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]- |
| Ixazomib |
| B-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]boronic acid |
2. Packaging
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping
4. Contact information
For more details, pls contact us freely.
Email address : Sun@fdachem.com
Mob: 86 13526505137
WhatsApp/Skype/Wechat/LINE: 86 13526505137
Company Profile Introduction
Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.
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- Since: 2023-02-10
- Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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