LL-00084282 | PI3Kδ/γ inhibitor | Probechem Biochemicals

Chemical Structure : LL-00084282

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LL-00084282 (LL00084282)

货号: PC-49531Not For Human Use, Lab Use Only.

LL-00084282 is a potent, selective and efficacious dual PI3Kδγ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.

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生物&药学活性

LL-00084282 is a potent, selective and efficacious dual PI3Kδ/γ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.
LL-00084282 demonstrated high selectivity against PI3Kα and PI3Kβ with IC50 values of 582.1 nM and 342.0 nM, respectively.
LL-00084282 displayed no significant binding on human GPCRs, ion-channels and kinase panels from Eurofins Discovery.
In contrast to selective PI3Kδ inhibitors, LL-00084282 showed superior and potent anticancer activity in both ABC- and GCB-DLBCL cell lines.
LL-00084282 demonstrated in-vivo efficacy in OCI-Ly10 and SU-DHL-6 xenografts with good tolerability.
LL-00084282 inhibited pro-inflammatory cytokine secretion and reduced basophil activation in human PBMCs, showing potential implications in immunoinflammatory conditions.

物理化学性质&存储条件

分子量	415.43
分子式	C22H18FN7O
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	(S)-2,4-diamino-6-((1-(7-fluoro-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile

参考文献

1. Mahip K Verma, et al. Biochem Biophys Res Commun. 2022 Dec 31;637:267-275.

LL-00084282 (LL00084282)

生物&药学活性

物理化学性质&存储条件

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LL-00084282 (LL00084282)

生物&药学活性

物理化学性质&存储条件

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