BRD8833 | BCR-ABL inhibitor, BCR-ABL Y253 phosphorylation inducer

Chemical Structure : BRD8833

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BRD8833 (BRD-8833)

货号: PC-26678Not For Human Use, Lab Use Only.

BRD8833 is a small molecule that induces BCR-ABL Y253 phosphorylation disrupts BCR-ABL signaling pathway.

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100 mg		Get quote

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生物&药学活性

BRD8833 is a small molecule that induces BCR-ABL Y253 phosphorylation disrupts BCR-ABL signaling pathway.
BRD8833 potently induces apoptosis of BCR-ABL-dependent cancer cells at a low nanomolar concentration.
BRD8833 shows potent cytotoxicity in K562 cells with EC50 of 69 nM.
BRD8833 dose-dependent cytotoxicity (EC50: 35-149 nM) for BCR-ABL positive CML cell lines (KCL22, BV-173, EM-2 and KYO-1), but not on HEK293T cells that lack BCR-ABL.
BRD8833 reduces the viability with an EC50 value of 280 nM in Ba/F3 cells expressing TEL-ABL, potently inhibits the viability of different oncogenic ABL-fusions.
BRD8833 exhibits high selectivity for CML cells dependent on ABL oncogenic fusions with minimal off-target effects on other cell lines.
BRD8833 is active in cells harboring a gatekeeper mutation (T315I), which renders active-site drugs (e.g., imatinib) ineffective, and in cells with other oncogenic ABL fusions (e.g., TEL-ABL) that are insensitive to approved drugs (e.g., asciminib).

物理化学性质&存储条件

分子量	844.58
分子式	C36H38Cl4N12O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2,2'-(((ethane-1,2-diylbis(oxy))bis(ethane-2,1-diyl))bis(azanediyl))bis(N-(1-(3,4-dichlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl)-4-methylpyrimidine-5-carboxamide)

参考文献

1. Merz ML, et al. ACS Cent Sci. 2026 Apr 9;12(4):473-483.

BRD8833 (BRD-8833)

生物&药学活性

物理化学性质&存储条件

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BRD8833 (BRD-8833)

生物&药学活性

物理化学性质&存储条件

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