For research use only. Not for therapeutic Use.
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL)[1].
SJ988497 (compound 7) increases cell permeability in the Caco-2 assay, with the apparent permeability coefficient (Papp) of 19.12 nm/s[1].
SJ988497 inhibits parental MHH-CALL-4 cells with an EC50 of 0.4 nM, inhibits CRBN-KD MHH–CALL-4 cells with an EC50 of 3456.2 nM, and can be blocked by 30 μM Lenalidomide (HY-A0003)[1].
SJ988497 (1 h, 1 μM) results in comparable JAK inhibition in MHH–CALL-4 cells[1].
SJ988497 (compound 7) (30 mg/kg, i.p.) reduces spleen size and tumor burdens, and is well tolerated with no weight loss or perturbation in blood count[1].
SJ988497 (10-100 mg/kg, i.p., twice daily) showed sustained in vivo exposure with the plasma concentration above the cellular 50% effective concentration value after 24 hour[1].
| Catalog Number | I042461 |
| CAS Number | 2595365-41-4 |
| Synonyms | N-[4-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]butyl]-4-[[4-(1-propylpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide |
| Molecular Formula | C36H36N10O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C36H36N10O5/c1-2-18-45-20-22(19-40-45)30-25-14-17-38-31(25)44-36(43-30)41-23-10-8-21(9-11-23)32(48)39-16-4-3-15-37-26-7-5-6-24-29(26)35(51)46(34(24)50)27-12-13-28(47)42-33(27)49/h5-11,14,17,19-20,27,37H,2-4,12-13,15-16,18H2,1H3,(H,39,48)(H,42,47,49)(H2,38,41,43,44) |
| InChIKey | MPFPDTOOHBZQJD-UHFFFAOYSA-N |
| SMILES | CCCN1C=C(C=N1)C2=C3C=CNC3=NC(=N2)NC4=CC=C(C=C4)C(=O)NCCCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O |
| Reference | [1]. Chang Y, et al. Degradation of Janus kinases in CRLF2-rearranged acute lymphoblastic leukemia. Blood. 2021 Dec 9;138(23):2313-2326. |
