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KA2507

Catalog No. T9148   CAS 1636894-46-6
Synonyms: KA-2507

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

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KA2507, CAS 1636894-46-6
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Purity 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.
In vitro KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition.
In vivo 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).[1]
Synonyms KA-2507
Molecular Weight 322.32
Formula C16H14N6O2
CAS No. 1636894-46-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

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

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Apostolia M Tsimberidou, 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 May 4.

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