I-BET567

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

I-BET567 是一种有效、具有口服活性 pan-BET 候选抑制剂，对 BRD4 BD1 和 BD2 的 pIC50s 分别为 6.9 和 7.2。I-BET567 已在肿瘤和炎症小鼠模型中已被证明有效。

I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM).Cell Viability Assay Cell Line:NMC line 11060 cells Concentration:1.5 nM-30 μM Incubation Time:72 hours Result:Significantly reduced cell growth.

I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg.Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle doga.a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2.Animal Model:NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells) Dosage:3, 10, and 30 mg/kg Administration:p.o. (once daily for 20 days Result:Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.

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Others

Other Targets

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1887237-54-8

359.81

C17H18ClN5O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (277.92 mM; 超声助溶 )

C[C@H]1C[C@@H](Nc2ncc(Cl)cn2)c2cc(ccc2N1C(C)=O)C(N)=O

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(-20℃)

With Ice Pack

≥ 2 years