| Bioactivity | PARP7-IN-14 (I-1) is a potent and selective PARP7 inhibitor with an IC50 value of 7.6 nM. PARP7-IN-14 has anticancer activity[1]. | ||||||||||||
| Invitro | PARP7-IN-14 (I-1) 作用于 CT26 细胞的 MTT IC50 值为 12.85 μM，具有一定的肿瘤抗增殖作用[1]。 PARP7-IN-14 (I-1)(0-4 μM)可促进 CT26 细胞系中 IFN-β 和 CXCL10 的 mRNA 表达水平并诱导 STAT1 磷酸化浓度依赖性增加[1]。 | ||||||||||||
| In Vivo | PARP7-IN-14 (I-1)(p.o., 25-100 mg/kg, twice daily, 14 days) 在 CT26 荷瘤小鼠中, 可以明显抑制剂肿瘤生长，与对照组相比，用 I-1 处理的小鼠平均肿瘤体积减少了 67%，且不会导致体重减轻或其他毒性迹象[1]。 | ||||||||||||
| Name | PARP7-IN-14 | ||||||||||||
| Formula | C21H24F6N8O2 | ||||||||||||
| Molar Mass | 534.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Hongfeng Gu, et al. Discovery of the Potent and Highly Selective PARP7 Inhibitor as a Novel Immunotherapeutic Agent for Tumors. J Med Chem. 2023 Jan 12;66(1):473-490. |