BLU0588 |
| Catalog No.GC73517 |
BLU0588 es un inhibide la cinasa PRKACA (proteína quinasa catalítica activpor camp-subunidad alfa), con una IC50 de 1 nM y una constante de disoci(Kd) de 4 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2810747-78-3
Sample solution is provided at 25 µL, 10mM.
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BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research.
BLU0588 (1.5 μM, 1 day or 14 days) reverses a FLC-specific gene signature, leading to downregulation of genes that are overexpressed in FLC (CPS1 and G6PC, top) and upregulation of genes that are underexpressed in FLC[1].BLU0588 (0-312.5 nM) reduces pVASP in FLC PDX cells in a dose-dependent manner[1].
BLU0588 (30-75 mg/kg, orally, once) can inhibit PRKACA, effectively inhibits downstream signaling of PRKACA, phosphorylated VASP levels returns to baseline levels by 24 hours[1]. The highest tolerated dose of BLU0588 for more than 3 weeks of continuous dosing was established as 30 mg/kg QD in mice[1].BLU0588 (30 mg/kg, orally, once daily, 34 days) can inhibits tumor growth in mice[1].
References:
[1]. Stefanie S. Schalm, et al. Evaluation of Protein Kinase cAMP-Activated Catalytic Subunit Alpha as a Therapeutic Target for Fibrolamellar Carcinoma. Gastro Hep Advances. Volume 2, Issue 3, 2023, Pages 307-321.
| Cas No. | 2810747-78-3 | SDF | |
| Formula | C26H25N5O | M.Wt | 423.51 |
| Solubility | DMSO : 83.33 mg/mL (196.76 mM; ultrasonic and warming and heat to 60°C) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3612 mL | 11.8061 mL | 23.6122 mL |
| 5 mM | 0.4722 mL | 2.3612 mL | 4.7224 mL |
| 10 mM | 0.2361 mL | 1.1806 mL | 2.3612 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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