CAS No. : 1072833-77-2

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000335
Synonyms:[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronic acid
Molecular Formula:C14H19BCl2N2O4
Molecular Weight:361.0
IC50:3.4 nM (20S proteasome ) [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000335
Cas No:1072833-77-2

MLN2238(Ixazomib) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively.
IC50 Value: 3.4 nM (20S proteasome ) [1]
Target: 20S proteasome
MLN2238 also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. MLN2238 is the biologically active form of MLN9708.
in vitro: MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. MLN2238 is a selective, potent, and reversible inhibitor of the proteasome in tumor cells. MLN2238 shows time-dependent reversible proteasome inhibition. Both MLN2238 and Bortezomib shows time-dependent reversible proteasome inhibition; however, the proteasome dissociation half-life for MLN2238 is determined to be 6-fold faster than that of Bortezomib (18 and 110 minutes, respectively). MLN2238 dissociates more rapidly from the proteasome than Bortezomib, consistent with faster recovery of proteasome activity observed in the Proteasome-Glo assay. MLN2238 has a greater overall tumor pharmacodynamic effect than Bortezomib as assessed by 20S inhibition [1]. MLN2238 is the biologically active form of MLN9708 [2]. MLN2238 can induce caspase-independent cell death in RRCL. MLN2238 (and to a much lesser degree bortezomib) reduced RRCL S phase and induced cell cycle arrest in the G2/M phase. Exposure of rituximab-chemotherapy-sensitive cell lines and RRCL to MLN2238 potentiated the cytotoxic effects of gemcitabine, doxorubicin, and paclitaxel and overcame resistance to chemotherapy in RRCL [3].
in vivo: MLN2238 shows greater maximum and sustained tumor proteasome inhibition compared with Bortezomib in xenograft models. These results confirm that the improved tumor exposure seen with MLN2238 translates into an improved tumor pharmacodynamic response both at the level of and downstream from the proteasome. MLN2238 shows antitumor activity in the CWR22 xenograft model. MLN2238 shows greater tumor pharmacodynamic responses in WSU-DLCL2 xenografts compared with Bortezomib. Similarly, Bortezomib treatment only led to a minor increase in GADD34 levels in WSU-DLCL2 xenograft tumors, whereas MLN2238 strongly induces its expression [1]. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with Bortezomib in both OCI-Ly10 and PHTX22L models [2].
Toxicity: N/A
Clinical trial: A Study of MLN-9708 in Adult Patients With Lymphoma. Phase 1

1:The combination of MLN2238 (ixazomib) with interferon-alpha results in enhanced cell death in melanoma. Suarez-Kelly LP, Kemper GM, Duggan MC, Stiff A, Noel TC, Markowitz J, Luedke EA, Yildiz VO, Yu L, Jaime-Ramirez AC, Karpa V, Zhang X, Carson WE 3rd.Oncotarget. 2016 Dec 6;7(49):81172-81186. doi: 10.18632/oncotarget.12791. PMID: 27783987 Free PMC Article
2:Comparison of antiproliferative and apoptotic effects of a novel proteasome inhibitor MLN2238 with bortezomib on K562 chronic myeloid leukemia cells. Engür S, Dikmen M, Öztürk Y.Immunopharmacol Immunotoxicol. 2016;38(2):87-97. doi: 10.3109/08923973.2015.1122616. Epub 2015 Dec 15. PMID: 26667773
3:MLN2238 synergizes BH3 mimetic ABT-263 in castration-resistant prostate cancer cells by induction of NOXA. Wei X, Zhou P, Lin X, Lin Y, Wu S, Diao P, Xie H, Xie K, Tang P.Tumour Biol. 2014 Oct;35(10):10213-21. doi: 10.1007/s13277-014-2333-y. Epub 2014 Jul 17. PMID: 25027405
4:The investigational agent MLN2238 induces apoptosis and is cytotoxic to CLL cells in vitro, as a single agent and in combination with other drugs. Paulus A, Masood A, Miller KC, Khan AN, Akhtar D, Advani P, Foran J, Rivera C, Roy V, Colon-Otero G, Chitta K, Chanan-Khan A.Br J Haematol. 2014 Apr;165(1):78-88. doi: 10.1111/bjh.12731. Epub 2014 Jan 27. PMID: 24467634
5: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. Gu JJ, Hernandez-Ilizaliturri FJ, Mavis C, Czuczman NM, Deeb G, Gibbs J, Skitzki JJ, Patil R, Czuczman MS.Anticancer Drugs. 2013 Nov;24(10):1030-8. doi: 10.1097/CAD.0000000000000008. PMID: 23995855
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