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A-1210477
CAS No. 1668553-26-1
A-1210477( A1210477 )
Catalog No. M12546 CAS No. 1668553-26-1
A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 31 | In Stock |
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| 5MG | 50 | In Stock |
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| 10MG | 87 | In Stock |
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| 25MG | 147 | In Stock |
|
| 50MG | 259 | In Stock |
|
| 100MG | 403 | In Stock |
|
| 500MG | 888 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameA-1210477
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NoteResearch use only, not for human use.
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Brief DescriptionA-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes.
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DescriptionA-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.
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In VitroA-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.
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In Vivo——
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SynonymsA1210477
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PathwayAngiogenesis
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TargetBcl-2
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RecptorMcl-1
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1668553-26-1
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Formula Weight850.0366
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Molecular FormulaC46H55N7O7S
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Purity>98% (HPLC)
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SolubilityDMSO: < 4.8 mg/mL
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SMILESO=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
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Chemical Name1H-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]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Leverson JD, et al. Cell Death Dis. 2015 Jan 15;6:e1590.
2. Xiao Y, et al. Mol Cancer Ther. 2015 Aug;14(8):1837-47.
3. Phillips DC, et al. Blood Cancer J. 2015 Nov 13;5:e368.
4. Karpel-Massler G, et al. Cancer Res. 2017 Jul 1;77(13):3513-3526.
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