Rohinitib 是一种有效的以及特异性的eIF4A抑制剂。Rohinitib 诱导急性髓系白血病 (AML) 细胞系的凋亡,并减轻在 AML 异种移植模型小鼠的白血病负担。Rohinitib 可用于 AML 的研究。
生物活性 | Rohinitib is a potent and specificeIF4Ainhibitor. Rohinitib induces cellapoptosisof acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML[1]. |
体外研究 (In Vitro) | Rohinitib (6.25-50 nM; 72 h) induces cell apoptosis of AML cell lines andFLT3-ITD-positive AML cell lines[1].Primary AML cells is more sensitive to Rohinitib (25 nM; 72 h) than normal bone marrow (BM) andFLT3-ITD-positive cells is more sensitive to Rohinitib thanFLT3wild-type AML cells[1].
Apoptosis Analysis[1] Cell Line: | AML cell lines | Concentration: | 6.25, 12.5, 25 and 50 nM | Incubation Time: | 72 h | Result: | Dose-dependently induced apoptosis of MOLM-13, MOLM-14, MV4;11, OCI-AML3, THP-1, HL-60, Kasumi-1 and NB4 cell lines. And significantly induced cell apoptosis ofFLT3-ITD,FLT3-ITD-expressing murine Ba/F3 and human OCI-AML3 cells. |
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体内研究 (In Vivo) | Rohinitib (0.75 and 1.0 mg/kg; s.c. once daily for 5 consecutive days until mice get moribund) shows anti-AML effects in vivo[1].
Animal Model: | Female NSG mice with AML xenografts generated by intravenous injections of MOLM-13 cells[1] | Dosage: | 0.75 and 1.0 mg/kg | Administration: | Subcutaneous injection; 0.75 and 1.0 mg/kg once daily 5 days a week until mice get moribund | Result: | Significantly reduced the leukemia burden, circulating and BM leukemic human CD45+cells. Dose-dependently prolonged the survival rate of mice. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 200 mg/mL(383.46 mM;Need ultrasonic) 配制储备液 1 mM | 1.9173 mL | 9.5866 mL | 19.1732 mL | 5 mM | 0.3835 mL | 1.9173 mL | 3.8346 mL | 10 mM | 0.1917 mL | 0.9587 mL | 1.9173 mL |
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