A-1210477 free base · Synonyms: A 1210477 · A1210477

A-1210477 is a potent and selective inhibitor of MCL-1.

For research use only. Not for human or veterinary use.

Target Bcl-2 Family Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

A-1210477 structure

CAS No.: 1668553-26-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 500.00	BP-02334-250mg	In stock	Get quote
500 mg	USD 750.00	BP-02334-500mg	In stock	Get quote
1 g	USD 1,250.00	BP-02334-1g	In stock	Get quote
5 g	Inquire	BP-02334-5g	In stock	Inquire
10 g	Inquire	BP-02334-10g	In stock	Inquire

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Description

A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.

Biological activity

A-1210477 causes a dose-dependent reduction in the amount of BIM co-immunoprecipitated with MCL-1, with an IC50 in the low-μM range. 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 measured in the same cell background. A-1210477 binds to MCL-1 selectively and with sufficient affinity to disrupt MCL-1-BIM complexes in living cells. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines demonstrated to be MCL-1 dependent by BH3 profiling or siRNA rescue experiments.

Identifiers

SMILES: CN(C)S(=O)(=O)N1CCN(CC1)C1=CC=C(OCC2=C(C(C)=NN2C)C2=CC=CC3=C2N(CCN2CCOCC2)C(C(O)=O)=C3CCCOC2=C3C=CC=CC3=CC=C2)C=C1
InChIKey: XMVAWGSQPHFXKU-UHFFFAOYSA-N

Specifications

MW (average): 850.0370
Formula: C₄₆H₅₅N₇O₇S
CAS No.: 1668553-26-1
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Leverson JD, 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. 2015 Jan 15;6:e1590.

[2]. Qing Wang, et al. A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. Oncol Lett. 2019 Nov;18(5):5481-5489.

Same target

Search Bcl-2 Family

Same research area

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