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首页-小分子抑制剂&激动剂-TGF-beta/Smad-TGF beta Receptor (TGFBR)-TP-0184
TP-0184

Chemical Structure : TP-0184

CAS No.: 1628870-27-8

TP-0184 (Itacnosertib, TP0184)

货号: PC-21414Not For Human Use, Lab Use Only.

Itacnosertib (TP-0184) is a novel potent, selective inhibitor of type I bone morphogenetic protein (BMP) receptor ACVR1 (activin A receptor-type 1, ALK2) and FLT3 with IC50 of 8.0 nM (ALK2).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Itacnosertib (TP-0184) is a novel potent, selective inhibitor of type I bone morphogenetic protein (BMP) receptor ACVR1 (activin A receptor-type 1, ALK2) and FLT3 with IC50 of 8.0 nM (ALK2).
TP-0184 binds to both ACVR1 and FLT3 with high affinity and inhibits FLT3/ACVR1 downstream signaling.
TP-0184 selectively caused growth arrest in FLT3-mutated AML cell lines.
Treatment with TP-0184 or in combination with BCL2 inhibitor, venetoclax dramatically inhibited leukemia growth in FLT3-mutated AML cell lines and patient-derived xenograft models in a dose-dependent manner.

物理化学性质&存储条件

分子量 468.57
分子式 C26H28N8O
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

N4-([2,2'-bipyridin]-3-yl)-N2-(3-methoxy-4-(4-methylpiperazin-1-yl)phenyl)pyrimidine-2,4-diamine

参考文献

1. Anudishi Tyagi, et al. Leukemia. 2023 Nov 25. doi: 10.1038/s41375-023-02086-6.

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