KME-2780 | IRAK1/4 inhibitor | Probechem Biochemicals

Chemical Structure : KME-2780

CAS No.: 2968466-26-2

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KME-2780 (KME2780)

货号: PC-21201Not For Human Use, Lab Use Only.

KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.

规格	价格	库存
5 mg	￥1680	In stock
10 mg	￥2580	In stock
25 mg	￥4580	In stock
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100 mg		Get quote

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生物&药学活性

KME-2780 (KME2780) is a potent and selective dual IRAK1 and IRAK4 (IRAK1/4) inhibitor with IC50 of 19 and 0.5 nM, respectively.
KME-2780 shows Kd values of 2.2 and 0.2 nM for IRAK1 and IRAK4, respectively.
KME-2780 is significantly more effective at suppressing TLR2-mediated activation of NF-κB and autophosphorylation of IRAK1 in AML cells as compared with the IRAK4 seleective inhibitor KME-3859.
KME-2780 downregulats genes in MAPK/AP1, ATF4, IGFBP, and EGFR signaling in AML cells.
KME-2780 suppresses eukemia stem/progenitor cells (LSPCs), suppresses OCI-AML3 cells, which is insensitive to the genetic inactivation of IRAK1 and IRAK4.
KME-2780 treatment also resulted in a greater expression of CD38, a glycoprotein expressed on mature immune cells.
KME-2780 (30 mg/kg, orally daily) suppresses MDS/AML in xenografted mice.

物理化学性质&存储条件

分子量	333.44
分子式	C20H23N5
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	(R)-6-(6-(1-methylcyclopropyl)imidazo[1,2-a]pyridin-3-yl)-N-(pyrrolidin-3-yl)pyridin-2-amine

参考文献

1. Bennett J, et al. Blood. 2023 Sep 14;142(11):989-1007.

KME-2780 (KME2780)

生物&药学活性

物理化学性质&存储条件

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KME-2780 (KME2780)

生物&药学活性

物理化学性质&存储条件

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