产品
编 号：F753993
分子式：C36H36N10O5
分子量：688.74
分子式：C36H36N10O5
分子量：688.74
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2595365-41-4
产品详情
生物活性：
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).
体内研究：
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.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.Animal Model:NSG mice inoculated by CL20SF2-Luc2aYFP cell (i.v.)
Dosage:30 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Reduced leukemia burden in bone marrow, blood, and spleen, as well as total body bioluminescent imaging.
体外研究：
SJ988497 (compound 7) increases cell permeability in the Caco-2 assay, with the apparent permeability coefficient (Papp) of 19.12 nm/s.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).SJ988497 (1 h, 1 μM) results in comparable JAK inhibition in MHH–CALL-4 cells.
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).
体内研究：
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.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.Animal Model:NSG mice inoculated by CL20SF2-Luc2aYFP cell (i.v.)
Dosage:30 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Reduced leukemia burden in bone marrow, blood, and spleen, as well as total body bioluminescent imaging.
体外研究：
SJ988497 (compound 7) increases cell permeability in the Caco-2 assay, with the apparent permeability coefficient (Papp) of 19.12 nm/s.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).SJ988497 (1 h, 1 μM) results in comparable JAK inhibition in MHH–CALL-4 cells.
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