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MedKoo product information:
MLN-2238
Description of
MLN-2238:
MLN-2238 is the biologically
active form of
MLN9708. MLN2238 has an improved
pharmacodynamic profile and antitumor activity compared with
bortezomib in both OCI-Ly10 and PHTX22L models. Although both
MLN2238 and bortezomib prolonged overall survival, reduced
splenomegaly, and attenuated IgG2a levels in the iMyc(Cα)/Bcl-X(L)
GEM model, only MLN2238 alleviated osteolytic bone disease in the
DP54-Luc model. The antitumor activity of MLN2238 in a variety of
mouse models of B-cell lymphoma and PCM, supporting its clinical
development.
MLN9708 is being evaluated in multiple phase I and I/II
trials. (source:
Clin Cancer Res. 2011 Dec 1;17(23):7313-23. Epub 2011 Sep 8.)
Current developer: Millennium Pharmaceuticals, Inc
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MedKoo Code#: 205857
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Name: MLN-2238
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CAS#:
1072833-77-2
Synonym:
MLN-2238; MLN-2238; MLN-2238.
IUPAC/Chemical name:
(R)-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)boronic
acid
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Chemical structure
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Theoretical analysis
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MedKoo Code#: 205857
Name: MLN-2238
CAS#: 1072833-77-2
Chemical Formula: C14H19BCl2N2O4
Exact Mass: 360.08149
Molecular Weight: 361.02866
Elemental Analysis: C, 46.58; H, 5.30; B,
2.99; Cl, 19.64; N, 7.76; O, 17.73
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Availability and price:
This agent is
available through custom synthesis.
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Highlights of recent research using this agent
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1: Mullard A. Next-generation proteasome blockers
promise safer cancer therapy. Nat Med. 2012 Jan 6;18(1):7. doi:
10.1038/nm0112-7a. PubMed PMID: 22227650.
2: Anderson KC. The 39th David A. Karnofsky Lecture: bench-to-bedside
translation of targeted therapies in multiple myeloma. J Clin Oncol.
2012 Feb 1;30(4):445-52. Epub 2012 Jan 3. PubMed PMID: 22215754.
3: Appel A. Drugs: More shots on target. Nature. 2011 Dec
14;480(7377):S40-2. doi: 10.1038/480S40a. PubMed PMID: 22169800.
4: Lee EC, Fitzgerald M, Bannerman B, Donelan J, Bano K, Terkelsen J,
Bradley DP, Subakan O, Silva MD, Liu R, Pickard M, Li Z, Tayber O, Li P,
Hales P, Carsillo M, Neppalli VT, Berger AJ, Kupperman E, Manfredi M,
Bolen JB, Van Ness B, Janz S. Antitumor activity of the investigational
proteasome inhibitor MLN9708 in mouse models of B-cell and plasma cell
malignancies. Clin Cancer Res. 2011 Dec 1;17(23):7313-23. Epub 2011 Sep
8. PubMed PMID: 21903769.
5: Chauhan D, Tian Z, Zhou B, Kuhn D, Orlowski R, Raje N, Richardson P,
Anderson KC. In vitro and in vivo selective antitumor activity of a
novel orally bioavailable proteasome inhibitor MLN9708 against multiple
myeloma cells. Clin Cancer Res. 2011 Aug 15;17(16):5311-21. doi:
10.1158/1078-0432.CCR-11-0476. Epub 2011 Jun 30. PubMed PMID: 21724551;
PubMed Central PMCID: PMC3156932.
6: Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu
J, Yang Y, Hales P, Bruzzese F, Liu J, Blank J, Garcia K, Tsu C, Dick L,
Fleming P, Yu L, Manfredi M, Rolfe M, Bolen J. Evaluation of the
proteasome inhibitor MLN9708 in preclinical models of human cancer.
Cancer Res. 2010 Mar 1;70(5):1970-80. Epub 2010 Feb 16. Erratum in:
Cancer Res. 2010 May 1;70(9):3853. Hales, Paul [added]. PubMed PMID:
20160034.
7: Dick LR, Fleming PE. Building on bortezomib: second-generation
proteasome inhibitors as anti-cancer therapy. Drug Discov Today. 2010
Mar;15(5-6):243-9. Epub 2010 Jan 29. Review. PubMed PMID: 20116451.
8: Marblestone JG. Ubiquitin Drug Discovery & Diagnostics 2009 - First
Annual Conference. IDrugs. 2009 Dec;12(12):750-3. PubMed PMID: 19943215.
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Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
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