QC-6352

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

QC-6352 是一种有效的选择性 KDM4 家族抑制剂。

QC-6352 is a potent and selective KDM4 family inhibitor with IC50 of 104, 56, 35, and 104 nM for KDM4A, KDM4B, KDM4C, and KDM4D, respectively; displays high selectivity over other KDM family members, with the exception of KDM5B (IC50=750 nM); shows a promising cellular potency (KYSE-150 EC50=3.5 nM, H3K36 MOA=1.5 nM); has excellent physical properties and drug-like characteristics, exhibits favorable in vivo efficacy in a breast cancer PDX model and reduces the tumor initiating cell populations which are associated with resistance to chemotherapy treatments.

QC6352 is a potent KDM4C inhibitor with an IC50 of 35±8 nM. In a concentration-dependent manner QC6352 dramatically reduces the sphere-forming capacity of BCSC1 and BCSC2. QC6352 blocks proliferation and self-renewal of BCSCs. As shown by western blot analysis the protein levels of (Epidermal growth factor receptor) EGFR are reduced in both BCSC1 and BCSC2 upon treatment with QC6352.

QC6352 strongly affects tumor growth and final tumor weight of both BCSC1 and BCSC2 xenografts. Treatment with QC6352 is well tolerated and does not affect body weight of the mice. Results demonstrate that treatment with the KDM4 inhibitor QC6352 blocks BCSC xenograft tumor growth.

QC6352

Chromatin/Epigenetic

Histone Demethylase

Histone Demethylase

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1851373-36-8

387.483

C24H25N3O2

>98% (HPLC)

DMSO : ≥ 25 mg/mL 64.52 mM

O=C(O)C1=CC=NC=C1NC[C@@H]2CCCC3=C2C=CC(N(C)C4=CC=CC=C4)=C3

(R)-3-(((6-(methyl(phenyl)amino)-1,2,3,4-tetrahydronaphthalen-1-yl)methyl)amino)isonicotinic acid

(-20℃)

With Ice Pack

≥ 2 years