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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.
M. Wt | 376.37 |
Formula | C20H16N4O4 |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 37.64 | 100 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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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