Ixazomib | Proteasome inhibitor

CAS:
 1072833-77-2
Catalog Number:
 10-5185

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Ixazomib (1072833-77-2) is a selective, potent, and reversible proteasome inhibitor, which targets the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50 of 3.4 nM) and the caspase-like (β1) site (IC50 of 31 nM).1 Ixazomib displays more potent, dose-dependent and time-dependent cytotoxicity and inhibition of cell proliferation than bortezomib.2 It is a clinically useful agent  (in cotreatment with other drugs) for multiple myeloma.3 It has also been shown to be effective in Light Chain (AL) Amyloidosis and is often used in combination with cyclophosphamide and dexamethasone.4

References/Citations:

  1. Gupta et al. (2018), Clinical Pharmacology of Ixazomib: The First Oral Proteasome Inhibitor; Clin. Pharmacokinet. 58 431
  2. Gu et al. (2013), MLN2238, a proteasome inhibitor, induces caspase-dependent cell death, cell cycle arrest, and potentiates the cytotoxic activity of chemotherapy agents in rituximab-chemotherapy-sensitive or rituximab-chemotherapy-resistant B-cell lymphoma preclinical models; Anticancer Drugs 24 1030
  3. Muz et al. (2016), Spotlight on ixazomib: potential in the treatment of multiple myeloma; Drug Des. Devel. Ther. 10 217
  4. Muchtar et al. (2022), Phase 2 trial of ixazomib, cyclophosphamide, and dexamethasone for previously untreated light chain amyloidosis.; Blood Adv. 6 5429
1072833-77-2, ixazomib, Ixazomib supplier, MLN2238, Proteasome inhibitor
CAS:
1072833-77-2
Catalog Number:
10-5185
Activity:
Proteasome inhibitor
Chemical Names:
(R)-(1-(2-(2,5-Dichlorobenzamido)acetamido)-3-methylbutyl)boronic acid
Alternate Name:
MLN2238
Molecular Weight:
361.03
Molecular Formula:

C14H19BCl2N2O4

Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
White to off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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Ixazomib (1072833-77-2) is a selective, potent, and reversible proteasome inhibitor, which targets the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50 of 3.4 nM) and the caspase-like (β1) site (IC50 of 31 nM).1 Ixazomib displays more potent, dose-dependent and time-dependent cytotoxicity and inhibition of cell proliferation than bortezomib.2 It is a clinically useful agent  (in cotreatment with other drugs) for multiple myeloma.3 It has also been shown to be effective in Light Chain (AL) Amyloidosis and is often used in combination with cyclophosphamide and dexamethasone.4

References/Citations:

  1. Gupta et al. (2018), Clinical Pharmacology of Ixazomib: The First Oral Proteasome Inhibitor; Clin. Pharmacokinet. 58 431
  2. Gu et al. (2013), MLN2238, a proteasome inhibitor, induces caspase-dependent cell death, cell cycle arrest, and potentiates the cytotoxic activity of chemotherapy agents in rituximab-chemotherapy-sensitive or rituximab-chemotherapy-resistant B-cell lymphoma preclinical models; Anticancer Drugs 24 1030
  3. Muz et al. (2016), Spotlight on ixazomib: potential in the treatment of multiple myeloma; Drug Des. Devel. Ther. 10 217
  4. Muchtar et al. (2022), Phase 2 trial of ixazomib, cyclophosphamide, and dexamethasone for previously untreated light chain amyloidosis.; Blood Adv. 6 5429

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