KA2507 monohydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

KA2507 monohydrochloride 

KA2507 hydrochloride 是一种高效、高选择性的 HDAC6 抑制剂 IC50=2.5 nM)，无明显毒性。KA2507 hydrochloride 具有抗肿瘤和免疫调节作用。

KA2507 monohydrochloride

KA2507 monohydrochloride Chemical Structure

规格 价格 是否有货
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KA2507 monohydrochloride 的其他形式现货产品:

KA2507

生物活性

KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects[1].

体外研究
(In Vitro)

KA2507 hydrochloride does not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition. The anti-proliferative effects are only observed at high concentrations of KA2507 hydrochloride, which combines with the increased acetylation of histone H3 suggests that the anti-proliferative effects of KA2507 hydrochloride are attributable to off-target inhibition of class I HDAC as well as HDAC6[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

KA2507 hydrochloride (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model[1].
KA2507 hydrochloride also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models[1].
Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 hydrochloride administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I[1].
KA2507 hydrochloride exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice, B16-F10 melanoma model[1]
Dosage: 100 mg/kg, 200 mg/kg,
Administration: P.o.; once a day for 20 days
Result: Inhibited tumor growth in the syngeneic B16-F10 mouse melanoma model.
Animal Model: Male C57BL/6 mice, B16-F10 melanoma model[1]
Dosage: 200 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Oral bioavailability (15%), Cmax (300 ng/mL).

Clinical Trial

分子量

358.78

Formula

C16H15ClN6O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献

  • [1]. Tsimberidou AM, et al. Preclinical Development and First-in-Human Study of KA2507, a Selective and Potent Inhibitor of Histone Deacetylase 6, for Patients with Refractory Solid Tumors. Clin Cancer Res. 2021;27(13):3584-3594.

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