SR-3029
Based on 2 publication(s) in Google Scholar
SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
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- Pureza: 99.73%
- No. CAS: 1454585-06-8
- Fòrmula: C23H19F3N8O
- Peso molecular:480.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) SR-3029
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Customer Validation & Images
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WB
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WB
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RT-PCR
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RT-PCR
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IHC
Actividad biológica
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CK1δ 44 nM (IC50) |
CDK6/cyclin D3 427 nM (IC50) |
CDK6/cyclin D1 428 nM (IC50) |
CDK4/cyclin D3 368 nM (IC50) |
CDK4/cyclin D1 576 nM (IC50) |
FLT3 3000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 5637 | EC50 |
6 nM
Compound: SR-3029
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Antiproliferative activity against human 5637 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human 5637 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 37204207] |
| MDA-MB-231 | EC50 |
26 nM
Compound: 13; SR-3029
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29289448] |
| T-24 | EC50 |
8 nM
Compound: SR-3029
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Antiproliferative activity against human T24 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human T24 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 37204207] |
| U2OS | EC50 |
9 nM
Compound: SR-3029
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Antiproliferative activity against human U2OS cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human U2OS cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 37204207] |
| UMUC3 | EC50 |
26 nM
Compound: SR-3029
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Antiproliferative activity against human UMUC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human UMUC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 37204207] |
SR-3029 is a potent CK1δ/CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively. SR-3029 is ATP competitive, with Kis of 97 nM for CK1δ/CK1ε. SR-3029 also blocks CDK6/cyclin D3, CDK6/cyclin D1, CDK4/cyclin D3, CDK4/cyclin D1 and FLT3, with IC50s of 427, 428, 368, 576, and 3000 nM, respectively. SR-3029 shows inhibitory effects on A375 cells, with an EC50 of 86 nM[1]. CK1δ is a necessary and sufficient driver of Wnt/β-catenin signaling in human breast cancer. SR-3029 shows less potent activities against MCF7 and T47D breast cancer cells and the MCF10A cell line, which express low amounts of CK1δ[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1454585-06-8
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Appearance Solid
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Peso molecular 480.45
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Fòrmula C23H19F3N8O
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Color White to pink
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SMILES
FC1=CC(N2C=NC3=C(NCC4=NC5=CC=C(F)C(F)=C5N4)N=C(N6CCOCC6)N=C23)=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
Tumor promoter TPA activates Wnt/β-catenin signaling in a casein kinase 1-dependent manner. [Abstract]2018 Aug 7;115(32):E7522-E7531. PMID: 30038030
SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]
TPA induces the phosphorylation of LRP6 and the formation of a CK1ε-LRP6-axin1 complex. (A) HEK293T and UACC903 cells cotransfected with CK1ε-GFP and LRP6 expression vectors are treated with 10 nM TPA for 6 h. Cell lysates are analyzed by immunoblotting. (B) HEK293T and UACC903 cells transfected with a CK1εexpression plasmid ae treated with or without 10 nM TPA for 6 h. (C) UACC903 cells are incubated with 10 nM TPA in the presence or absence of 60 nM SR3029 for 6 h.
SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]
SR3029 suppresses TPA-induced skin tumor formation in vivo via blockade of Wnt/β-catenin signaling in mouse skin two-stage chemical carcinogenesis. Fifteen mice per group are initiated with DMBA, followed by repetitive applications of TPA alone or together with SR3029 in acetone twice a week for 18 wk. Expression levels of β-catenin, active β-catenin, CK1ε, CK1δ, and LRP6 in tumor samples are visualized after immunoblotting.
SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]
SR3029 suppresses TPA-induced skin tumor formation in vivo via blockade of Wnt/β-catenin signaling in mouse skin two-stage chemical carcinogenesis. Fifteen mice per group are initiated with DMBA, followed by repetitive applications of TPA alone or together with SR3029 in acetone twice a week for 18 wk. The mRNA expression levels of CD44, cyclin D1, and Fosb in tumor tissuesare quantitated by real-time PCR.
SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]
TPA increases the expression of Wnt target genes. HEK293T and UACC903 cells are treated for 24 h with or without 10 nM TPA in the presence or absence of increasing concentrations of SR3029 as indicated. Quantitative PCR analysis is conducted to detect the mRNA expression of CD44, cyclin D1, and DKK1.
SR-3029 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]
SR3029 suppresses TPA-induced skin tumor formation in vivo via blockade of Wnt/β-catenin signaling in mouse skin two-stage chemical carcinogenesis. Fifteen mice per group are initiated with DMBA, followed by repetitive applications of TPA alone or together with SR3029 in acetone twice a week for 18 wk. Hematoxylin/eosin staining and immunohistochemistry staining using antibodies specific for Ki-67, β-catenin, active β-catenin, CK1ε, and CK1δ.
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Solvente y solubilidad
DMSO : ≥ 30 mg/mL (62.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Protocolo
Briefly, final assay concentrations for CK1δ, Ulight peptide substrate (ULight-Topo-Ila(Thr1342) peptide) and ATP are 2 nM, 200 nM and 20 μM respectively. The reaction is performed at room temperature in a 10 μL final volume (384-well low volume plate) containing the following: 50 mM Hepes, pH 7.5, 5 mM MgCl2, 0.1 mg/mL bovine serum albumin, 1 mM dl-dithiothreitol, 0.01% Triton X-100 and 1% DMSO. After 10 min, the reaction is terminated by addition of 10 μL of 4 nM Eu-anti-p-Topo-Ila in Lance Detection Buffer. The fluorescent signal is detected using a plate reader. 10 point does-response curves with 3-fold dilutions starting from 10 μM for each compound (SR-3029) is generated in duplicate and data fit to a four parameter logistic[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Human A375 melanoma cells are cultured in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum, 1% penicillin/streptomycin and 1× MEM Non-Essential Amino Acids at 37°C, 5% CO2. To evaluate the anti-proliferative activity of newly synthesized CK1δ/ε inhibitors, each compound (SR-3029) is subjected to MTT assays against A375 melanoma cells and their EC50 values are determined. Briefly, A375 melanoma cells are plated into a 96-well plate and treated with a series of concentrations of each new inhibitor, vehicle (DMSO) or with SR-3029 or SR-1277 (positive controls). MTT assays are performed four days after treatment and data are analyzed using the GraphPad Prism5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Stable pools of MDA-MB-231-Luc, MDA-MB-231, MDA-MB-468, SKBR3, or BT474 cells are established by injection of 2 × 106 cancer cells into the mammary fat pads of 6-week-old female athymic nude mice. Establishment of BCM-4013 patient-derived xenografts is performed. Briefly, fresh xenograft tumor fragments (∼1 mm3) are transplanted into the cleared mammary fat pad of recipient SCID/Bg mice. Mice are treated with SR-3029 or vehicle (10:10:80, DMSO:Tween-80:Water) at 20 mg/kg daily by i.p. injection. Tumor volumes are measured as the indicated intervals using calipers or by luminescence imaging with the IVIS 100 imager after subcutaneous injection of luciferin (15 mg/mL). Average radiance (p/s/cm2/sr) is determined from tumor region-of-interest (ROI) using Living-Image analysis software[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bibian M, et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80. [Content Brief]
[2]. Rosenberg LH, et al. Therapeutic targeting of casein kinase 1δ in breast cancer. Sci Transl Med. 2015 Dec 16;7(318):318ra202. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0814 mL | 10.4069 mL | 20.8138 mL | 52.0345 mL |
| 5 mM | 0.4163 mL | 2.0814 mL | 4.1628 mL | 10.4069 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0814 mL | 5.2035 mL | |
| 15 mM | 0.1388 mL | 0.6938 mL | 1.3876 mL | 3.4690 mL | |
| 20 mM | 0.1041 mL | 0.5203 mL | 1.0407 mL | 2.6017 mL | |
| 25 mM | 0.0833 mL | 0.4163 mL | 0.8326 mL | 2.0814 mL | |
| 30 mM | 0.0694 mL | 0.3469 mL | 0.6938 mL | 1.7345 mL | |
| 40 mM | 0.0520 mL | 0.2602 mL | 0.5203 mL | 1.3009 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4163 mL | 1.0407 mL | |
| 60 mM | 0.0347 mL | 0.1734 mL | 0.3469 mL | 0.8672 mL |
SR-3029 Related Classifications
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