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- 文献和实验
- 技术资料
- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
LY2606368 dihydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1234015-54-3
- 规格：
2 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 2 mg | 产品价格： | ￥700.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥1300.0 |
| 规格： | 10 mg | 产品价格： | ￥2300.0 |
| 规格： | 25 mg | 产品价格： | ￥4600.0 |
| 规格： | 50 mg | 产品价格： | ￥7800.0 |
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Prexasertib dihydrochloride
CAS No. : 1234015-54-3
MCE 国际站：Prexasertib dihydrochloride
产品活性：Prexasertib dihydrochloride (LY2606368 dihydrochloride) 是一种选择性的，ATP 竞争性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂，Ki 为 0.9 nM，IC50 为 <1 nM。Prexasertib dihydrochloride 抑制 CHK2 (IC50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib dihydrochloride 引起双链 DNA 断裂和复制突变，导致细胞凋亡 (apoptosis)。Prexasertib dihydrochloride 显示有效的抗肿瘤活性。
研究领域：Cell Cycle/DNA Damage | Apoptosis
作用靶点：Checkpoint Kinase (Chk) | Apoptosis
In Vitro: Prexasertib dihydrochloride (LY2606368 dihydrochloride) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). LY2606368 requires CDC25A and CDK2 to cause DNA damage.
?Prexasertib dihydrochloride (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells.
?Prexasertib dihydrochloride (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells.
?Prexasertib dihydrochloride (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells.
? ?Prexasertib dihydrochloride (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA.
In Vivo: Prexasertib dihydrochloride (LY2606368 dihydrochloride; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts.
?Prexasertib dihydrochloride (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8).
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