MLN9708 Inhibitor CAS No. 1201902-80-8

Cat. No.	Name	Size	Price
KI1454	MLN9708	5 mg	$330
	MLN9708	10 mg	$624
	MLN9708	50 mg	$1896
	MLN9708	200 mg	$4828

Chemical Characteristic

Product Name	MLN9708
Synonyms	Ixazomib
CAS No.	1201902-80-8
Molecular Weight	517.12
Formula	C₂₀H₂₃BCl₂N₂O₉
Chemical Name	4-Carboxy-2-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-6-oxo-1,3,2-dioxaborinane-4-acetic acid
Smiles	O1B(OC(CC1=O)(CC(=O)O)C(=O)O)C(CC(C)C)NC(=O)CNC(=O)c1c(ccc(c1)Cl)Cl
Chemical Structure

Biological activities

MLN9708 is a selective, potent, and reversible proteasome inhibitor. MLN9708 inhibits chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 and 0.93 nM, respectively. MLN9708 also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 0.031 and 3.5 µM, respectively. The proteasome dissociation half-life (t1/2) for MLN2238 is about 6-foldfaster than that of bortezomib. MLN9708 strongly inhibits TNF-α-induced activation of the NF-κB pathway in tumor cells.^[1] MLN2238 treatment predominantly inhibits chymotrypsin-like activity of the proteasome and induces accumulation of ubiquitinated proteins in multiple myeloma (MM) cells. MLN2238 also inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies without affecting the viability of normal cells. In animal tumor model studies, MLN2238 is well tolerated and inhibits tumor growth with significantly reduced tumor recurrence.^[2] In vivo, MLN2238 shows both greater maximum and sustained tumor proteasome inhibition compared with bortezomib in both CWR22 and WSU-DLCL2 xenografts models.^[1] Besides, MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with bortezomib in both OCI-Ly10 and PHTX22L models.^[3]

Protocols

In vitro: MLN9708 is dissolved in DMSO.^[4]

References

[1] Kupperman E, et al. Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer. Cancer Res. 2010, 70(5): 1970-1980. [2] Chauhan D , et al. In vitro and in vivo selective antitumor activity of a novel orally bioavailable proteasome inhibitor MLN9708 against multiple myeloma cells. Clin Cancer Res. 2011, 17(16): 5311-5321. [3] Lee EC, et al. Antitumor activity of the investigational proteasome inhibitor MLN9708 in mouse models of B-cell and plasma cell malignancies. Clin Cancer Res. 2011, 17(23): 7313-7323. [4] Anshu A, et al. Novel proteasome-inhibitory syrbactin analogs inducing endoplasmic reticulum stress and apoptosis in hematological tumor cell lines. Biochem Pharmacol. 2011, 82(6): 600-609.

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