Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
In vitro growth of human or mouse cancer cells is not inhibited by KA2507 at dosages that specifically block HDAC6 [1].
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ln Vivo |
KA2507 (100-200 mg/kg; oral; daily; for 20 days) suppresses tumor growth in the syngeneic B16-F10 mouse melanoma model [1]. KA2507 has shown anti-tumor activity in CT26 and MC38 colorectal cancer models [1]. Analysis of tumor samples also demonstrated modulation of anti-tumor immune biomarkers at effective doses, with KA2507 administration leading to reduced activation of STAT3 (measured by phosphorylated STAT3, an important suppressor of anti-tumor immune responses), reduced PD-L1 expression, decreased PD- L1 expression increases MHC class I expression [1]. KA2507 has poor oral bioavailability (15% in mice) and Cmax (300 ng/mL in mice) after oral treatment (200 mg/kg in mice) [1].
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Animal Protocol |
Animal/Disease Models: Male C57BL/6 mouse, B16-F10 melanoma model [1]
Doses: 100 mg/kg, 200 mg/kg, 200 mg/kg Route of Administration: po (oral gavage), daily, for 20 days Experimental Results: Shows anti-tumor efficacy. Animal/Disease Models: Male C57BL/6 mice [1] Doses: 200 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Oral Experimental Results: Oral bioavailability (15%), Cmax (300 ng/mL). |
References |
[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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Molecular Formula |
C16H14N6O2
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Molecular Weight |
322.3214
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CAS # |
1636894-46-6
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Related CAS # |
KA2507 monohydrochloride;2972712-63-1
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SMILES |
O=C(C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N(C1C([H])=NC([H])=C([H])N=1)C1C([H])=NC([H])=C([H])N=1)N([H])O[H]
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~206.84 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.1025 mL | 15.5125 mL | 31.0251 mL | |
5 mM | 0.6205 mL | 3.1025 mL | 6.2050 mL | |
10 mM | 0.3103 mL | 1.5513 mL | 3.1025 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.