YX-2-107
Based on 1 publication(s) in Google Scholar
YX-2-107 is a PROTAC (IC50= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph+ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).
(Pink: CDK6 ligand (HY-50767); Blue: Cereblon ligand (HY-103596); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.60%
- CAS. Nr.: 2417408-46-7
- Formel: C45H51N11O9
- Molecular Weight:889.95
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) YX-2-107
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CDK6 4.4 nM (IC50) |
In Vitro
YX-2-107 (2000 nM; 48 h) shows inhibition of S phase in Ph+ BV173 and SUP-B15 cells[1].
YX-2-107 (0, 1.6, 8, 40, 200, 1000 nM;4 h) selectively degrades CDK6 in BV173 cells[1].
YX-2-107 (2000 nM; 72 h) inhibits RB phosphorylation and FOXM1 expression in Ph+ BV173 and SUP-B15 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Ph+ BV173 and SUP-B15 cells
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Concentration:2000 nM
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Incubation Time:48 h
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Result:Inhibited S-phase entry.
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Cell Line:Ph+ BV173 and SUP-B15 cells
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Concentration:2000 nM
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Incubation Time:72 h
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Result:Inhibited the phosphorylation of RB and the expression of FOXM1.
In Vivo
YX-2-107 (150 mg/kg; i.p.; single daily for 3 days) is pharmacologically active in suppressing Ph+ ALL proliferation in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NRG-SGM3 mice (Ph+ ALL xenografts model)[1].
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Dosage:150 mg/kg
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Administration:Intraperitoneal injection; single daily for 3 days
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Result:Suppressed the percentage of primary Ph+ ALL S-phase cells, the expression of CDK4/6-regulated phospho-RB and, to a lesser degree, FOXM1, and induced the selective CDK6 degradation.
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Animal Model:C57BL/6j mice[1].
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; single
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Result:
1.19 Pharmacokinetic Parameters of YX-2-107 in C57BL/6j mice [1].
IP (10 mg/kg) Tmax (h) 0.5 Cmax (ng/mL) 660 AUC0-t (ng/mL·h) 815 AUC0-∞ (ng/mL·h) 987
Chemical Information
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CAS. Nr. 2417408-46-7
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Appearance Solid
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Molecular Weight 889.95
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Formel C45H51N11O9
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Color Yellow to orange
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCC(NCCCCNCC(N4CCN(CC4)C5=CN=C(NC6=NC(N(C7CCCC7)C(C(C(C)=O)=C8C)=O)=C8C=N6)C=C5)=O)=O)=CC=C3)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (112.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.1237 mL | 5.6183 mL | 11.2366 mL | 28.0915 mL |
| 5 mM | 0.2247 mL | 1.1237 mL | 2.2473 mL | 5.6183 mL | |
| 10 mM | 0.1124 mL | 0.5618 mL | 1.1237 mL | 2.8091 mL | |
| 15 mM | 0.0749 mL | 0.3746 mL | 0.7491 mL | 1.8728 mL | |
| 20 mM | 0.0562 mL | 0.2809 mL | 0.5618 mL | 1.4046 mL | |
| 25 mM | 0.0449 mL | 0.2247 mL | 0.4495 mL | 1.1237 mL | |
| 30 mM | 0.0375 mL | 0.1873 mL | 0.3746 mL | 0.9364 mL | |
| 40 mM | 0.0281 mL | 0.1405 mL | 0.2809 mL | 0.7023 mL | |
| 50 mM | 0.0225 mL | 0.1124 mL | 0.2247 mL | 0.5618 mL | |
| 60 mM | 0.0187 mL | 0.0936 mL | 0.1873 mL | 0.4682 mL | |
| 80 mM | 0.0140 mL | 0.0702 mL | 0.1405 mL | 0.3511 mL | |
| 100 mM | 0.0112 mL | 0.0562 mL | 0.1124 mL | 0.2809 mL |
YX-2-107 Related Classifications
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