2. Cell Cycle/DNA Damage Apoptosis
  3. Checkpoint Kinase (Chk) Apoptosis
  4. Prexasertib Mesylate Hydrate

Prexasertib Mesylate Hydrate  (Synonyms: LY2606368 Mesylate Hydrate; LY2940930)

目录号: HY-18174B
产品使用指南

摩尔计算器

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。

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Prexasertib Mesylate Hydrate Chemical Structure

Prexasertib Mesylate Hydrate Chemical Structure

CAS No. : 1234015-57-6

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Prexasertib Mesylate Hydrate 的其他形式现货产品:

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Other Forms of Prexasertib Mesylate Hydrate:

Prexasertib Mesylate Hydrate 相关抗体

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查看 Checkpoint Kinase (Chk) 亚型特异性产品:

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Chk1 Chk2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Prexasertib Mesylate Hydrate 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 33, 100 nM
Incubation Time: For 7 hours
Result: Had an IC50 of 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) (IC50 of 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

Prexasertib Mesylate Hydrate 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

Prexasertib Mesylate1234015-57-6LY2606368 Mesylate LY2940930LY2940930LY 2940930LY-2940930Checkpoint Kinase (Chk)ApoptosisATP-competitiveRSK1double-strandedDNAreplicationMELKSIKBRSK2ARK5CDC25ACDK2HeLaautophosphorylationS296S516H2AXHT-29Inhibitorinhibitorinhibit

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