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OM137
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
OM137图片
CAS NO:292170-13-9

产品介绍

生物活性

OM137 is an inhibitor of aurora kinases; inhibitor of spindle checkpoint. OM137 is an aminothiazole derivative, which functions to override the spindle checkpoint primarily through inhibition of the Aurora kinases (mitotic kinases). OM137 is a more potent inhibitor of Aurora B compared with Aurora Ain vitro, consistent with the effects of OM137 on checkpoint function in living cells. The compound has some CDK1 inhibitory activity, but is likely that the major mode by which OM137 drives mitotic exit of cells arrested in M phase via the spindle checkpoint is through its inhibitory activity against Aurora B kinase. The compound is less potent than N-[4-[(6,7-Dimethoxy-4-quinazolinyl)amino]phenyl]benzamide hydrochloride (Sigma Cat. D6068), which is more suited forin vitrotesting due to low solubility and high serum binding. OM137 is less potent than selective Aurora A inhibitor, cyclopropanecarboxylic acid {3-[4-(3-trifluoromethyl-phenylamino)-pyrimidin-2-ylamino]-phenyl}-amide (Sigma Cat. C2368).


化学数据

分子量306.34
分子式C13H14N4O3S
CAS号292170-13-9
纯度>98%
溶解性(25°C)DMSO: ≥10 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

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)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM3.2643 mL16.3217 mL32.6435 mL
5 mM0.6529 mL3.2643 mL6.5287 mL
10 mM0.3264 mL1.6322 mL3.2643 mL