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.
For research use only. We do not sell to patients.
- CAS No.: 2972712-63-1
- Formula: C16H15ClN6O2
- Molecular Weight:358.78
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Storage:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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 No. 2972712-63-1
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Appearance Solid
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Molecular Weight 358.78
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Purity & Documentation
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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)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KA2507 monohydrochloride Related Classifications
HY-138799A Related Classifications
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