您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Prexasertib Mesylate Hydrate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Prexasertib Mesylate Hydrate
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。
Prexasertib Mesylate Hydrate图片
CAS NO:1234015-57-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
LY2606368 Mesylate Hydrate
LY2940930
产品介绍
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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 mesylate hydrate 抑制 CHK2 (IC50=8 nM) 和 RSK1 (IC50=9 nM)。Prexasertib Mesylate Hydrate 引起双链 DNA 断裂和复制突变,导致细胞凋亡 (apoptosis)。Prexasertib Mesylate Hydrate 显示有效的抗肿瘤活性。
生物活性

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generationcheckpoint kinase 1 (CHK1)inhibitor with aKiof 0.9 nM and anIC50of<1 nm. prexasertib mesylate hydrate inhibitsCHK2(IC50=8 nM) andRSK1(IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting inapoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity[1][2].

IC50& Target

Chk1

0.9 nM (Ki)

Chk1

<1 nM (IC50)

Chk2

8 nM (IC50)

体外研究
(In Vitro)

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 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[1].
Prexasertib Mesylate Hydrate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1].
Prexasertib Mesylate Hydrate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1].
Prexasertib Mesylate Hydrate (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[1].
Prexasertib Mesylate Hydrate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib Mesylate Hydrate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA[1].

Cell Cycle Analysis[1]

Cell Line:HeLa cells
Concentration:33, 100 nM
Incubation Time:For 7 hours
Result:Had an IC50of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis.

Western Blot Analysis[1]

Cell Line:HT-29 cells
Concentration:8, 16, 31, 63, 125, 250 nM
Incubation Time:Pre-treated for 15 minutes
Result:Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC50of less than 31 nM) in HT-29 cells.
体内研究
(In Vivo)

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts[1].
Prexasertib Mesylate Hydrate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1].

Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
Dosage:1, 3.3, or 10 mg/kg
Administration:SC; twice daily for 3 days, rest 4 days; for three cycles
Result:Caused statistically significant tumor growth inhibition (up to 72.3%).
Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
Dosage:15 mg/kg (Pharmacokinetic Analysis)
Administration:SC (200 μL)
Result:CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures.
Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
Clinical Trial
分子量

479.51

Formula

C19H25N7O6S

CAS 号

1234015-57-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.