KA2507 monohydrochloride
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.
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- CAS. Nr.: 2972712-63-1
- Formel: C16H15ClN6O2
- Molecular Weight:358.78
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Speicherung:
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)
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice, B16-F10 melanoma model[1]
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Dosage:100 mg/kg, 200 mg/kg,
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Administration:P.o.; once a day for 20 days
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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]
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Dosage:200 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral administration
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Result:Oral bioavailability (15%), Cmax (300 ng/mL).
Chemical Information
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CAS. Nr. 2972712-63-1
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Appearance Solid
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Molecular Weight 358.78
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Formel C16H15ClN6O2
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Color Off-white to light yellow
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SMILES
O=C(NO)C1=CC=C(CN(C2=NC=CN=C2)C3=NC=CN=C3)C=C1.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
KA2507 monohydrochloride Related Classifications
HY-138799A Related Classifications
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