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Purity: ≥98%
SR-3029 is a novel, potent, highly kinase selective and ATP competitive CK1δ and CK1ε (casein kinase 1δ/1ε) inhibitor with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases. SR-2890 and SR-3029 have IC₅₀ ≤ 50 nM versus CK1δ. The two lead compounds have ≤100 nM EC50 values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines.
| ln Vitro |
SR-3029 is a strong CK1δ/CK1ε inhibitor, with an IC50 of 44 nM and 260 nM, respectively. SR-3029 exhibits ATP competition, as evidenced by its 97 nM Ki value for CK1δ/CK1ε. Moreover, SR-3029 inhibits FLT3, CDK6/cyclin D1, CDK6/cyclin D1, and CDK4/cyclin D3, with IC50 values of 427, 428, 368, 576, and 3000 nM, respectively. A375 cells are inhibited by SR-3029, with an EC50 of 86 nM[1]. In human breast cancer, CK1δ is a sufficient and essential driver of Wnt/β-catenin signaling. SR-3029 demonstrates negligible efficacy against MCF7, T47D, and MCF10A cell lines, all of which have low levels of CK1δ expression [2].
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| ln Vivo |
at orthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3, and BT474 (HER2+) tumor xenografts, SR-3029 (20 mg/kg ip daily) showed anticancer effects. It was also effective at modest doses and showed no overt harm to rats. In primary patient-derived xenograft (PDX) models, SR-3029 (20 mg/kg ip daily) also significantly reduces tumor growth. Furthermore, SR-3029 (20 mg/kg, intraperitoneal injection) significantly decreased the expression of nuclear β-catenin in mice tumors [2].
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| References |
[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.
[2]. Rosenberg LH, et al. Therapeutic targeting of casein kinase 1δ in breast cancer. Sci Transl Med. 2015 Dec 16;7(318):318ra202 |
| Molecular Formula |
C23H19F3N8O
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|---|---|
| Molecular Weight |
480.4452
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| CAS # |
1454585-06-8
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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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| InChi Key |
CEBMEQPREMCWOL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H19F3N8O/c24-13-2-1-3-14(10-13)34-12-28-20-21(31-23(32-22(20)34)33-6-8-35-9-7-33)27-11-17-29-16-5-4-15(25)18(26)19(16)30-17/h1-5,10,12H,6-9,11H2,(H,29,30)(H,27,31,32)
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| Chemical Name |
6,7-Difluoro-1H-benzoimidazol-2-ylmethyl)-[9-(3-fluoro-phenyl)-2-morpholin-4-yl-9H-purin-6-yl]-amine
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| Synonyms |
SR-3029; SR 3029; SR3029.
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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 : ≥ 30 mg/mL (~62.44 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0814 mL | 10.4069 mL | 20.8138 mL | |
| 5 mM | 0.4163 mL | 2.0814 mL | 4.1628 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0814 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.
 CK1δis a clinically relevant and effective target for select breast cancer subtypes.Sci Transl Med.2015 Dec 16;7(318):318ra202. |
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 Modulation of the Wnt/β-catenin pathway is a biomarker for CK1δ activity and inhibition.Sci Transl Med.2015 Dec 16;7(318):318ra202. |
 Silencing or inhibition of CK1δ provokes breast tumor regression and blocks growth of PDX breast models.Sci Transl Med.2015 Dec 16;7(318):318ra202. |
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