1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. KA2507 monohydrochloride

KA2507 monohydrochloride 

Cat. No.: HY-138799A
Handling Instructions

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.

For research use only. We do not sell to patients.

KA2507 monohydrochloride Chemical Structure

KA2507 monohydrochloride Chemical Structure

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Solution
10 mM * 1 mL in DMSO USD 385 Ask For Quote & Lead Time
Solid
5 mg USD 350 Ask For Quote & Lead Time

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Description

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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE 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).
Molecular Weight

358.78

Formula

C₁₆H₁₅ClN₆O₂

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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Product Name:
KA2507 monohydrochloride
Cat. No.:
HY-138799A
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