| Size | Price | Stock | Qty |
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| Targets |
CaMK II ULK1 26.6 nM (IC50)
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| ln Vitro |
XST-14 has been shown to inhibit various enzymes, including ULK1 (IC50 = 13.6 nM), MAP2K1/MEK1 (IC50 = 721.8 nM), MAPK14/p38 alpha (IC50 = 283.9 nM), TGFBR2 (IC50 = 809.3 nM), ACVR1/ALK2 (IC50 = 183.8 nM), ULK2 (IC50 = 70.9 nM), and CAMK2A (IC50 = 66.3 nM). Cell proliferative activity is reduced by XST-14 (20-80 μM) for a 24-hour period[1]. In HepG2 and human primary HCC cells, XST-14 (5 μM) causes apoptosis for a duration of 24 hours[1]. CHO cells producing GFP-LC3 steadily thanks to LC3-II[1]. XST-14 (5 μM) suppresses the phosphorylation of PIK3C3 at Ser249 and BECN1 at Ser15 after 12 hours[1].
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| ln Vivo |
In nude mice, XST-14 (15, 30 mg/kg/day; IP) exhibits anti-HCC efficacies, leading to reduced tumor weights and inhibited HCC cell proliferation in tumors[1]. T1/2 values for mg/kg for IV and 10 mg/kg for IP are 2.69 and 2.31 hours, respectively[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: HepG2 and human primary cells Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced apoptosis in HepG2 and human primary HCC cells. Cell Autophagy Assay[1] Cell Types: CHO, HepG2 cells stably expressing GFP -LC3 Tested Concentrations: 5 μM Incubation Duration: 12 hrs (hours) Experimental Results: Strongly inhibited the conversion of LC3-I to LC3-II in CHO cells. Dramatically diminished the number of GFP-LC3 puncta in HepG2 cells. diminished autophagosome formation and blocked autophagosome/lysosome fusion in HepG2 cells. Western Blot Analysis[1] Cell Types: HepG2 cells Tested Concentrations: 5 μM Incubation Duration: 12 hrs (hours) Experimental Results: Inhibited the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1. |
| Animal Protocol |
Animal/Disease Models: Nude mice bearing HepG2 tumor xenografts[1]
Doses: 15, 30 mg/kg Route of Administration: IP; daily; for 4 consecutive weeks Experimental Results: Displayed anti-HCC efficacies, resulting in diminished tumor weights and suppressed tumor growth of HCC cells in nude mice. Animal/Disease Models: SD (Sprague-Dawley) rat[1] Doses: 2 mg/kg for IV; 10 mg/kg for IP (pharmacokinetic/PK Analysis) Route of Administration: IV or IP Experimental Results: Had a T1/2 of 2.31 hrs (hours), a CL of 26.28 mL/min·kg, and and an AUC of 1269 hr·ng/mL for IV. Had a T1/2 of 2.69 hrs (hours), a Cmax of 2033 ng/mL, and an AUC of 5979 hr •ng/mL for IP. |
| References |
[1]. Si-Tu Xue, et al. The role of the key autophagy kinase ULK1 in hepatocellular carcinoma and its validation as a treatment target . Autophagy. 2020 Oct;16(10):1823-1837.
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| Molecular Formula |
C16H21NO4
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|---|---|
| Molecular Weight |
291.34
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| CAS # |
2607143-50-8
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| SMILES |
CC(C)OC1C2C=C(NC=2C=C(OC(C)C)C=1)C(OC)=O
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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 |
| 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 : 250 mg/mL (858.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.14 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4324 mL | 17.1621 mL | 34.3242 mL | |
| 5 mM | 0.6865 mL | 3.4324 mL | 6.8648 mL | |
| 10 mM | 0.3432 mL | 1.7162 mL | 3.4324 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.
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