KA2507

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

KA2507 是一种有效的选择性 HDAC6 抑制剂，IC50 为 2.5nM。

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition.

KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model.KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models.Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 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.KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg). Animal Model:Male C57BL/6 mice, B16-F10 melanoma model Dosage:100 mg/kg, 200 mg/kg, 200 mg/kg Administration:Oral gavage, daily, for 20 days Result:Demonstrated antitumor efficacy.Animal Model:Male C57BL/6 mice Dosage:200 mg/kg (Pharmacokinetic Analysis)Administration:Oral administration Result:Oral bioavailability (15%), Cmax (300 ng/mL).

——

Cell Cycle/DNA Damage

HDAC

HDAC6| HDAC8

——

——

1636894-46-6

322.32

C16H14N6O2

>98% (HPLC)

DMSO : 60 mg/mL (186.15 mM; Need ultrasonic)

O=C(NO)C1=CC=C(CN(C2=NC=CN=C2)C3=NC=CN=C3)C=C1

——

(-20℃)

With Ice Pack

≥ 2 years