生物活性
PD-173955是src酪氨酸激酶抑制剂。PD173955抑制Bcr-Abl依赖的细胞生长。PD173955显示G（1）中的细胞周期停滞。PD173955在Bcr-Abl的激酶抑制测定中的IC（50）为1-2 nM，在细胞生长测定中，其抑制Bcr-Abl依赖性底物酪氨酸磷酸化。 PD173955抑制试剂盒配体依赖性c-kit自磷酸化（IC（50）=约25 nM）和试剂盒配体依赖性M07e细胞增殖（IC（50）= 40 nM），但对白介素3依赖性（IC （50）= 250 nM）或粒细胞巨噬细胞集落刺激因子（IC（50）= 1 microM）依赖性细胞生长。
靶点信息
化学数据
| 目录号 | A13120 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 443.35 |
| Formula | C21H16Cl2N4OS |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 260415-63-2 |
| Synonyms | PD 173955; PD-173955 |
| SMILES | CN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=CC=C3Cl)Cl)NC4=CC(=CC=C4)SC |
溶解度
| In vitro | DMSO | Warmed: 13 mg/mL (29.32 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 22.56 mL | 112.78 mL | 225.56 mL |
| 0.5 mM | 4.51 mL | 22.56 mL | 45.11 mL |
| 1 mM | 2.26 mL | 11.28 mL | 22.56 mL |
| 5 mM | 0.45 mL | 2.26 mL | 4.51 mL |
*The above data is based on the productmolecular weight 443.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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