A selective Mcl-1 inhibitor
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Product Categories

Product Type

Small Molecule Modulators
Small Molecule Inhibitors

Research Area

Cancer
Cell Death
Apoptosis

Application

A-1210477

Item No. 21113

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
1668553-26-1
Molecular Formula
C46H55N7O7S
Formula Weight
850.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: SlightlyDMSO: SlightlyEthanol: Slightly
SMILES
CN(C)S(N1CCN(C2=CC=C(OCC3=C(C4=CC=CC5=C4N(CCN6CCOCC6)C(C(O)=O)=C5CCCOC7=C(C=CC=C8)C8=CC=C7)C(C)=NN3C)C=C2)CC1)(=O)=O
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    A-1210477 is an inhibitor of the antiapoptotic Bcl-2 family protein myeloid cell leukemia-1 (Mcl-1; Ki = 0.43 nM and IC50 = 26.2 nM) that demonstrates >100-fold selectivity over other Bcl-2 family members (Kis > 0.66 µM for Bcl-2, Bcl-XL, Bcl-W, and Bfl-1).1,2,3 It has been shown to disrupt the interaction between Mcl-1 and pro-apoptotic BIM, inducing the hallmarks of apoptosis in Mcl-1-dependent multiple myeloma and non-small cell lung cancer cell lines.1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Leverson, J.D., Zhang, H., Chen, J., et al. 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. 6, e1590 (2015).

    2. Bruncko, M., Wang, L., Sheppard, G.S., et al. Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity. J. Med. Chem. 58(5), 2180-2194 (2015).

    3. Opfeman, J.T. Attacking cancer’s Achilles heel: Antagonism of anti-apoptotic BCL-2 family members. FEBS J. 283(14), 2661-2675 (2016).