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BOC Sciences |
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1-631-485-4226; 16314854226 |
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info@bocsci.com |
KA2507 monohydrochloride manufacturers
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| | KA2507 monohydrochloride Basic information |
| | KA2507 monohydrochloride Chemical Properties |
| form | Solid | | color | Off-white to light yellow |
| | KA2507 monohydrochloride Usage And Synthesis |
| Uses | 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]. | | 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].
| 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.
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| 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).
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| | References | [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. DOI:10.1158/1078-0432.CCR-21-0238 |
| | KA2507 monohydrochloride Preparation Products And Raw materials |
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