1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)
  3. Prexasertib

Prexasertib (Synonyms: LY2606368)

製品番号: HY-18174 純度: 98.22%
取扱説明書

Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.

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Prexasertib 構造式

Prexasertib 構造式

CAS 番号 : 1234015-52-1

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 176 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 160 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 260 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 520 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 750 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1200 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Prexasertib:

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Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示:

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製品説明

Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.

IC50 & Target[1]

Chk1

0.9 nM (Ki)

Chk1

<1 nM (IC50)

Chk2

8 nM (IC50)

体外実験

Prexasertib (LY2606368) is a potent and selective ATP competitive inhibitor of Chk1, with an IC50 of <1 nM, and also inhibits CHK2, with an IC50 of 8 nM. Prexasertib has an EC50 of 1 nM for CHK1 activity through autophosphorylation of serine 296 and <31 nM for HT-29 CHK2 autophosphorylation (S516). Prexasertib potently abrogates the G2-M checkpoint activated by NSC 123127 in p53-deficient HeLa cells with an EC50 of 9 nM. However, 100 nM Prexasertib does not inhibit PMA-stimulated RSK but instead weakly stimulates phosphorylation of S6 on serines 235/236. Prexasertib is broadly antiproliferative with IC50s of 3 nM, 3 nM, 10 nM, 37 nM, and 68 nM against U-2 OS, Calu-6, HT-29, HeLa, and NCI-H460 cell lines, respectively. Prexasertib (4 nM) 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 (LY2606368; 25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. Prexasertib (20 nM) inhibits HR repair capacity DR-GFP cells. Prexasertib (5 nM) in combination with PARP inhibitor BMN673, displays synergistic anticancer effects in gastric cancer cells[2].

体内実験

Prexasertib (LY2606368; 15 mg/kg, s.c.) significantly inhibits tumor growth in xenograft tumor models with less animal weight loss[1]. Prexasertib (LY2606368; 2 mg/kg, s.c.) and BMN673 combination has synergistic anticancer effect in gastric cancer PDX model, and the effect is higher than that of one drug alone[2].

臨床実験
分子量

365.39

分子式

C₁₈H₁₉N₇O₂

CAS 番号

1234015-52-1

SMILES

NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 16.67 mg/mL (45.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7368 mL 13.6840 mL 27.3680 mL
5 mM 0.5474 mL 2.7368 mL 5.4736 mL
10 mM 0.2737 mL 1.3684 mL 2.7368 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (4.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

Proliferation inhibition effect of Chk1 ablation, IR sensitivity, anticancer effect of BMN673 and Prexasertib are detected by MTS Cell Proliferation Colorimetric Assay Kit. Cells are seeded into 96 wells cell culture plate, then treated with indicated experiment conditions, then added 20 μL MTS reagent to each well subsequently, after incubated for 2 hours, cell viability of each well is detected on microplate reader at a wavelength of 490 nM[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[1]

Female CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Vehicle consisting of 20% Captisol pH4 or Prexasertib is administered by subcutaneous injection in a volume of 200 μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS-MS system. The xenograft tissue is promptly removed and prepared. Lysates are analyzed by immunoblot analysis for protein phosphorylation levels. Group means, SEs and P values are calculated using Kronos.

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

PrexasertibLY2606368LY 2606368LY-2606368Checkpoint Kinase (Chk)Inhibitorinhibitorinhibit

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製品名:
Prexasertib
製品番号:
HY-18174
数量:
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