生物活性
SB431542是一种有效的，选择性的ALK5抑制剂，IC50为94 nM，对ALK5的作用比对p38、 MAPK和其他激酶强100倍。SB-431542作用于A498细胞无细胞毒性，LD50大于30 μM。 SB-431542也抑制ALK4和ALK7，这两种含有磷酸化Smad2。SB-431542对ALK1, ALK2, ALK3,和ALK6抑制作用不大, 这四种含磷酸化Smad1。
化学数据
| 分子量 | 384.39 |
| 分子式 | C22H16N4O3 |
| CAS号 | 301836-41-9 |
| 纯度 | 99.83% |
| 溶解性（25°C） | DMSO 40 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 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | human DCs |
| 方法 | Effects of SB-431542 on murine BM-DCs and human DCs. DCs were incubated in 96-well plates (5x104 cells/200 μl/well) with SB-431542 or vehicle alone and LPS in the presence of LPS at different concentrations in triplicates, and then examined for expression of co-stimulatory molecules using FACSCalibur. After 24 h of incubation, the cells were examined for surface expression of CD86 or CD83 within the CD11c+ populations, and the supernatants were tested for cytokine production by enzyme-linked immunosorbent assay (ELISA). Following 24 h of incubation with a test drug, BM-DCs were incubated for 10 min with 5 mg/ml of fluorescein isothiocyanate (FITC)-conjugated dextran (DX) (70,000 Dalton molecular weight, Sigma) at 4?C or 37?C, washed extensively, and then examined for FITC signals by CD11c+ cells. After drug pretreatment, BM-DC preparations (derived from BALB/c mice) were washed 3 times and then co-cultured in 96 round-bottom well plates at 4 different cell densities (0.3-10x103 cells/well) with splenic T cells purified from C57BL/6 mice (5x104 cells/well). The magnitude of T cell proliferation was assessed by 3H-thymidine uptake on day 4. Human DC cultures derived from PBMCs were examined for surface phenotype within the CD11c+ population and cytokine production by ELISA as well as for allogeneic mixed lymphocyte reaction. |
| 浓度 | 0~10 μM |
| 处理时间 | 24 hr |
| 动物实验 |
|---|
| 动物模型 | BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells |
| 配制 | normal saline |
| 剂量 | 1 μM (100μL) |
| 给药处理 | directly injected into peritoneal cavity |
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 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 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 / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6015 mL | 13.0076 mL | 26.0152 mL |
| 5 mM | 0.5203 mL | 2.6015 mL | 5.203 mL |
| 10 mM | 0.2602 mL | 1.3008 mL | 2.6015 mL |
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