RSH-7

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RSH-7 是一种有效的 BTK 和 FLT3 抑制剂，IC50 分别为 47、12 nM。RSH-7 诱导细胞凋亡 (apoptosis) 并显示抗增殖活性。RSH-7 抑制 BTK 和 FLT3 信号转导并显示出抗肿瘤活性。

RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.

RSH-7 (1-1000 nM; 72 h) shows antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively.RSH-7 (30, 150, 750 nM; 72 h) decreases the expression of p-BTK (TYR223), p-PLCγ(Tyr1217), p-FLT3 (Tyr589), p-STAT5 (TYR694) in a dose-dependent manner.RSH-7 (30, 150, 750 nM; 72 h) induces apoptosis and increases the expression of BAX, p53, cleaved caspase 3 in a dose dependen manner in jeko-1 cells..Cell Viability Assay Cell Line:Jeko-1, MV-4-11, Molt4, K562 cells Concentration:1-1000 nM Incubation Time:72 h Result:Showed antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively.Western Blot Analysis Cell Line:jeko-1 cells Concentration:30, 150, 750 nM Incubation Time:72 h Result:Reduced both BTK, PLCγ2, FLT3 and STAT5 phosphorylation in a dose-dependent manner.Apoptosis Analysis Cell Line:jeko-1 cellsConcentration:30, 150, 750 nM Incubation Time:72 h Result:Dose-dependently induced cell apoptosis and upregulated the expression of pro-apoptotic protein BAX, p53, cleaved caspase 3.

RSH-7 (25, 50 mg/kg; i.p.; daily for 16 days) shows anti-tumor activity with significantly and dose-dependently suppresses the tumor growth in mouse.Animal Model:Female NOD/SCID mice (jeko-1 cell-inoculated xenograft NOD/SCID mice models)Dosage:25, 50 mg/kg Administration:I.p.; daily for 16 days Result:Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) values of 66.95% and 79.78% at doses of 25 and 50 mg/kg,Animal Model:Female NOD/SCID mice (MV4-11 cell-inoculated xenograft NOD/SCID mice models)Dosage:10, 20 mg/kg Administration:I.p.; daily for 21 days Result:Significantly and dose-dependently suppressed the tumor growth with the TGI rates of 74.23% and 94.84% at the dosage of 10 and 20 mg/kg, respectively.

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Apoptosis

Apoptosis

Apoptosis | FLT | BTK

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2764609-97-2

436.49

C22H25FN8O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (190.91 mM; 超声助溶 )

N(C1=C(C(NN)=O)C=CC=C1)C2=NC(NC3=CC=C(C=C3)N4CCN(C)CC4)=NC=C2F

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(-20℃)

With Ice Pack

≥ 2 years