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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
- CAS号：
2595365-41-4
- 规格：
1 mg
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SJ988497
CAS No. : 2595365-41-4
MCE 国际站：SJ988497
产品活性：SJ988497 是一种 PROTAC JAK2 降解剂。SJ988497 可有效地抑制 CRLF2 重排 (CRLF2r) 细胞的增殖并降解 CRBN 新底物 GSPT1。SJ988497 由 Ruxolitinib (HY-50856) 衍生物、连接子和 CRBN 配体 Pomalidomide 组成。 SJ988497 可用于急性淋巴细胞白血病 (ALL) 的研究。
研究领域：PROTAC | JAK/STAT Signaling | Stem Cell/Wnt | Epigenetics | Protein Tyrosine Kinase/RTK
In Vitro: 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.
In Vivo: 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.
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, Wang YT, Ma J, Zhang P, Zhang TD, Chen SJ, Chen Z, Wang ZY. Use of arsenic trioxide in the treatment of acute promyelocytic leuke mia (APL):ⅠAs-2O-3 exerts dose dependent dual effects on APL cells. Blood,1997;89:3354-3360 [7] Konig A, Wrazel L, Warrell
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