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]-1H-indole-2-carboxylic acid

Name	Abbvie Mcl-1 Inhibitor
Synonyms	CS-2151 CS-2202 A1210477 A-1210477 A 1210477 Abbvie Mcl-1 Inhibitor BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101 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 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]-1H-indole-2-carboxylic acid 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]-
CAS	1668553-26-1

Molecular Formula	C46H55N7O7S
Molar Mass	850.04
Density	1.32±0.1 g/cm3(Predicted)
Boling Point	1027.4±65.0 °C(Predicted)
Solubility	DMSO: < 4.8 mg/mL
pKa	4.43±0.30(Predicted)
Storage Condition	Sealed in dry,Store in freezer, under -20°C
In vitro study	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 IC 50 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 IC 50 <10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines.

Last Update：2024-01-02 23:10:35

biological activity	A-1210477 is a potent, selective MCL-1 inhibitor with a Ki value of 0.45 nM. A- 1210477 specifically binds MCL-1 and promotes cancer cell apoptosis in A MCL-1 dependent manner.
Target	Mcl-1 0.45 nM (Ki) Bcl-2 132 nM (Ki) bfl -1 660 nM (Ki) Bcl-W 2280 nM (Ki) apotosis
in vitro study	A- 1210477 (10 μμm) reduce 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 inhibitors MCL-1-NOXA interactions with an IC 50 of approval 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 IC 50 <10 μM, confirming that A- 1210477 can kill MCL-1-dependent cell lines.

Last Update：2024-04-10 22:29:15

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CAS: 1668553-26-1
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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]-1H-indole-2-carboxylic acid Request for Quotation