WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407156
CAS#: 1668553-26-1
Description: A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines. A-1210477 synergizes with the BCL-2/BCL-XL inhibitor navitoclax to kill a variety of cancer cell lines. A-1210477 is a potential therapeutics for the treatment of cancer. The anti-apoptotic protein MCL-1 is a key regulator of cancer cell survival and a known resistance factor for small-molecule BCL-2 family inhibitors such as ABT-263 (navitoclax), making it an attractive therapeutic target.
MedKoo Cat#: 407156
Name: A-1210477
CAS#: 1668553-26-1
Chemical Formula: C46H55N7O7S
Exact Mass: 849.38837
Molecular Weight: 850.05
Elemental Analysis: C, 65.00; H, 6.52; N, 11.53; O, 13.17; S, 3.77
Synonym: A-1210477; A 1210477; A1210477.
IUPAC/Chemical Name: 7-(5-((4-(4-(N,N-dimethylsulfamoyl)piperazin-1-yl)phenoxy)methyl)-1,3-dimethyl-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid
InChi Key: XMVAWGSQPHFXKU-UHFFFAOYSA-N
InChi Code: InChI=1S/C46H55N7O7S/c1-33-43(41(49(4)47-33)32-60-36-19-17-35(18-20-36)51-22-24-52(25-23-51)61(56,57)48(2)3)40-14-8-13-38-39(15-9-29-59-42-16-7-11-34-10-5-6-12-37(34)42)45(46(54)55)53(44(38)40)26-21-50-27-30-58-31-28-50/h5-8,10-14,16-20H,9,15,21-32H2,1-4H3,(H,54,55)
SMILES Code: O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C(C=CC=C4)C4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O
1: Xiao Y, Nimmer P, Sheppard GS, Bruncko M, Hessler P, Lu X, Roberts-Rapp L,
Pappano WN, Elmore SW, Souers AJ, Leverson JD, Phillips DC. MCL-1 Is a Key
Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency
Utilizing a Highly Selective Small Molecule Inhibitor. Mol Cancer Ther. 2015
Aug;14(8):1837-47. doi: 10.1158/1535-7163.MCT-14-0928. Epub 2015 May 26. PubMed
PMID: 26013319.
2: Leverson JD, Zhang H, Chen J, Tahir SK, Phillips DC, Xue J, Nimmer P, Jin S,
Smith M, Xiao Y, Kovar P, Tanaka A, Bruncko M, Sheppard GS, Wang L, Gierke S,
Kategaya L, Anderson DJ, Wong C, Eastham-Anderson J, Ludlam MJ, Sampath D,
Fairbrother WJ, Wertz I, Rosenberg SH, Tse C, Elmore SW, Souers AJ. Potent and
selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell
killing activity as single agents and in combination with ABT-263 (navitoclax).
Cell Death Dis. 2015 Jan 15;6:e1590. doi: 10.1038/cddis.2014.561. PubMed PMID:
25590800.
