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生物活性
SGI-1776 is a ATP-competitive imidazo[1,2-b]pyridazine small molecule that specifically inhibits Pim-1, Pim-2, Pim-3, Flt-3 and haspin with IC50 values of 7, 363, 69, 44 and 34 nM, respectively. SGI-1776 concentration-dependently induces apoptosis in CLL lymphocytes and AML cell lines, and that mechanism involves Mcl-1 reduction through the inhibition of new RNA synthesis [1-2].
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体外研究
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体内研究
30% propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)
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激酶实验
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细胞实验
0.1, 0.3, 1, 3, -10μM
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动物实验
75 mg/kg和200 mg/kg 口服处理
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Chen LS, et al. Blood, 2011, 118(3), 693-702.
[2] Batra V, et al. Initial testing (stage 1) of SGI-1776, a PIM1 kinase inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer, 2012, 59(4), 749-752.
分子式
C20H22F3N5O |
分子量
405.42 |
CAS号
1025065-69-3 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
>80 mg/mL |
Water
<1 mg/mL |
Ethanol
>80 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
| NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
| NCT01239108 | Relapsed/Refractory Leukemias | Drug: SGI-1776 | Astex Pharmaceuticals | Phase 1 | 2010-10-01 | 2012-09-06 |
| NCT00848601 | Prostate Cancer|Non-Hodgkins Lymphoma | Drug: SGI-1776 | Astex Pharmaceuticals | Phase 1 | 2009-02-01 | 2011-12-01 |
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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