CTX-712 |
Catalog No.GC65023
One-Click Copy Product Info
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CTX-712 es un potente inhibidor de la quinasa similar al CDC2(CLK) conun valor IC50 de1.4nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2144751-78-8
Sample solution is provided at 25 µL, 10mM.
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CTX-712 es un potente inhibidor de la quinasa similar al CDC2(CLK) conun valor IC50 de1.4nM [1].CLK está asocida con diversas enfermedades neurodegenerativas,regulación metabólica e infecciones virales[2]. CTX-712 puede inhibir la supervivencia al cáncer y el crecimiento de las células cancerosas[3].
In vitro, después de 6 horas de tratamiento con CTX-712 en las células MOLM13,los niveles de fosforilación de SRSF2, SRSF4,y SRSF6 en las células disminuyeron de forma dependiente d ela dosis y se indujo la apoptosis.72 horas de tratamiento con CTX-712 inhibiron la proliferación d elíneas celulares de leucemia mieoide aguda (U937, THP1, MOLM13), con IC50 valores de 71.3±12.5nM, 147±16.1nM, y 35.5±2.3nM, respectivamente [4]. CTX-712 también inhibía la proliferación de las células myeloides humanas K562 y MV-4-11,con valores de IC50 valores de 0.15μM y 0.036μM, respectivamente.El valor IC50 de CTX-712 para las células de leuc emia mieloide aguda primaria (LMA) fue de 0.078μM,lo que indica su efecto antileucemia[3].
In vivo, la adeministración oral de CTX-712 (6.25-12.5mg/kg/día) durante 2 semanas inhibió la testosterona inhibiendo el tamaño tumoral en los ratones con síndrome mielodisplásico(MDS) y leucemia mieloide aguda (LMA),y mejora la tasa de supervivencia[3].
References:
[1] Tang J, Xie Y, Huang J, et al. A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing. Bioorg Med Chem. 2022;70:116921.
[2] Qin Z, Qin L, Feng X, Li Z, Bian J. Development of Cdc2-like Kinase 2 Inhibitors: Achievements and Future Directions. J Med Chem. 2021 Sep 23;64(18):13191-13211.
[3] Yoda A, Morishita D, Mizutani A, et al. CTX-712, a Novel Clk inhibitor targeting myeloid neoplasms with SRSF2 mutation[J]. Blood, 2019, 134: 404.
[4] Yang H, Fang Z, Wei Y, et al. CDC2-like Kinases (CLKs) Inhibition As a Novel Targeted Therapeutic Strategy in Myelodysplastic Syndromes (MDS)[J]. Blood, 2024, 144: 6691.
| Experimentos con animales [1]: | |
Modelos animales | Los ratones modelo AML/MDS |
Método de preparación | Estableció los 13 modelos de tumor xenoinjerto(PDX) derivados de las células del síndrome mielodisplásico/leucemia mieloide aguda.Investigaron a fondo el efecto de CTX-712 sobre el crecimiento tumoral in vivo,y se administraron diferentes dosis de CTX-712 (6.25, 12.5mg/kg/día)Tras do semanas de tratamiento,se midió el volumen tumoral (en milímetros cúbicos),junto con la tasa de supervivencia de los ratones. |
Forma de dosificación | 6.25, 12.5mg/kg/día durante 2 semanas; oral |
Áreas de aplicación | Entre los 5 ratones tratados con el régimen de dosis elevada(12,5 mg/kg),4 lograron una remisión completa (los tumores se redujeron completamente a un tamaño indetectable).Dos semanas depués del tratamiento con CTX-712,el volumen tumoral de los ratones modelo mutantes de SRSF2 P95L disminuyó signifcativamente,y CTX-712 también aumnetó significativamente la tasa de supervivencia de los ratones modelo SRSF2 P95L. |
References: | |
| Cas No. | 2144751-78-8 | SDF | |
| Formula | C19H17FN8O2 | M.Wt | 408.39 |
| Solubility | Storage | Store at -20°C,protect from light | |
| 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 | 2.4486 mL | 12.2432 mL | 24.4864 mL |
| 5 mM | 489.7 μL | 2.4486 mL | 4.8973 mL |
| 10 mM | 244.9 μL | 1.2243 mL | 2.4486 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)