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Submit ReviewSJ 3149 is a potent and selective CK1α molecular glue Degrader (DC50 = 3.7 nM; Dmax 95% in MOLM-13 cells). SJ 3149 induced near-complete degradation of the CK1α protein (DC50 = 6 nM at 4 hours). Potently inhibits the viability of MOLM-13 cells (IC50 = 13 nM). SJ 3149 displays a broad antiproliferative activity profile on a panel of acute leukemia and solid tumor cell lines. In vivo, SJ 3149 degrades CK1α protein levels in NSG mice transplanted with MOLM-13 cells. SJ 3149 shows 76% orally bioavailability.
Sold under license from St. Jude Children's Research Hospital.
分子量 | 376.37 |
公式 | C20H16N4O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 3026986-17-1 |
PubChem ID | 168511381 |
InChI Key | AJUZTJBGJWQZFW-UHFFFAOYSA-N |
Smiles | O=C1NC(C(CC1)N2C(C3=CC=C(NC4=NOC5=C4C=CC=C5)C=C3C2)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 37.64 | 100 |
以下数据基于产品分子量 376.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.66 mL | 13.28 mL | 26.57 mL |
5 mM | 0.53 mL | 2.66 mL | 5.31 mL |
10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Nishiguchi et al (2024) Selective CK1a degraders exert antiproliferative activity against a broad range of human cancer cell lines. Nat.Commun. 15 482 PMID: 38228616
If you know of a relevant reference for SJ 3149, please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including: