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250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
At concentrations that are specific for inhibiting HDAC6, KA2507 hydrochloride did not prevent the in vitro growth of human or animal cancer cells. Because the anti-proliferative effects of KA2507 hydrochloride are only seen at high concentrations, along with the increased acetylation of histone H3, it is possible that the inhibitory effects of KA2507 hydrochloride are due to off-target inhibition of both class I HDAC and HDAC6[1].
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ln Vivo |
In the syngeneic B16-F10 mouse melanoma model, KA2507 hydrochloride (100–200 mg/kg; po; daily; for 20 days) suppresses tumor growth[1]. The CT26 and MC38 colorectal cancer models show antitumor efficaciousness in response to KA2507 hydrochloride as well[1]. Tumor sample analysis also reveals modulation of biomarkers of antitumor immunity at effective dosing; administration of KA2507 hydrochloride results in decreased PD-L1 expression, increased MHC class I expression, and decreased STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response)[1]. Following oral dosing (mice 200 mg/kg), KA2507 hydrochloride shows poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL)[1].
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Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice, B16-F10 melanoma model[1]
Doses: 100 mg/kg, 200 mg/kg, Route of Administration: Po; one time/day for 20 days Experimental Results: Inhibited tumor growth in the syngeneic B16-F10 mouse melanoma model. Animal/Disease Models: Male C57BL/6 mice, B16-F10 melanoma model[1] Doses: 200 mg/kg (pharmacokinetic/PK Analysis) Route of Administration: Oral administration Experimental Results: Oral bioavailability (15%), Cmax (300 ng/mL). |
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.
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Molecular Formula |
C16H15CLN6O2
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Molecular Weight |
358.78
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CAS # |
2972712-63-1
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Related CAS # |
KA2507;1636894-46-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7872 mL | 13.9361 mL | 27.8722 mL | |
5 mM | 0.5574 mL | 2.7872 mL | 5.5744 mL | |
10 mM | 0.2787 mL | 1.3936 mL | 2.7872 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.