A-1210477

Research use only, not for human use.

A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes.

A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes, shows much weaker against Bcl-2 (Ki=132 nM) and Bcl-XL (Ki>660 nM); induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines, synergizes with the BCL-2/BCL-XL inhibitor navitoclax to kill a variety of cancer cell lines; also enhances cobimetinib-induced apoptosis in vitro.

A-1210477 (10?μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1?μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC50<10?μM, confirming that A-1210477 can kill MCL-1-dependent cell lines.

——

A1210477

Angiogenesis

Bcl-2

Mcl-1

Cancer

——

1668553-26-1

850.0366

C46H55N7O7S

>98% (HPLC)

DMSO: < 4.8 mg/mL

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

1H-Indole-2-carboxylic acid, 7-[5-[[4-[4-[(dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-

(-20℃)

With Ice Pack

≥ 2 years