Prexasertib

SKU: orb1302963

Description

Prexasertib

Research Area

Cell Biology

Key Properties

• CAS Number: 1234015-52-1
• MW: 365.39
• Purity: 97.30%
• Formula: C₁₈H₁₉N₇O₂
• SMILES: COc1cccc(OCCCN)c1-c1cc(Nc2cnc(cn2)C#N)n[nH]1
• Target: Apoptosis,Chk
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.74 mM);DMSO:22 mg/mL (60.21 mM)

Bioactivity

• Target IC50:
  Ramos cells:0.004 μM|RPMI8226 cells:0.048 μM|Chk1 < nM|Chk1:0.9 nM (Ki)|MV-4-11 cells:0.004 μM|Chk2:8 nM|Z-138 cells:0.033 μM|CHO cells:20 μM|HEK293 cells:385.98 nM|G2-M checkpoint:9 nM (EC50)|JeKo-1 cells:0.004 μM
• In Vivo:
  METHODS: To stud the antitumor activity of Prexasertib, mice were Subcutaneously injected with Prexasertib (1-10 mg/kg) twice a day for 3 consecutive days followed by a 4-day rest. For three weeks. Results: Prexasertib inhibite the growth of tumor xenografts.
• In Vitro:
  METHODS: Human JeKo1, MV4-11, Ramos, RPMI-8226, Z-138 cells were treated with Prexasertib (0 50 μM) for 72 h, and cell growth Inhibition was measured by a CellTiter 96 Aqueous One Solution reagent based assay. Results: Prexasertib inhibited JeKo1 IC50 0.004 μM), MV4-11 IC50 0.004 μM), Ramos IC50 0.004 μM), RPMI-8226 IC50 0.048 μM), Z-138 IC50 0.033) μM) cell growth.
• Cell Research:
  LY2606368 is broadly ant Proliferative with IC50 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 LY2606368 (25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. LY2606368 (20 nM) inhibits HR repair capacity DR-GFP cells.
• Animal Research:
  LY2606368 is formulated in Vehicle consisting of 20% Captisol.F Male CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of × 0^6 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 Each approximately 150 mm3 in size the animals are andomized by tumor size and body weight, and placed into their respective treatment groups. Vehicle consisting of 20% Captisol pH4 or LY2606368 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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Checkpoint Kinase (Chk), Chk2, Chk1, CDC25A, CDK2, DNA, double-stranded, BRSK2, Apoptosis, autophosphorylation, ARK5, ATP-competitive, MELK, Inhibitor, HeLa, HT-29, H2AX, LY 2606368, LY2606368, LY-2606368, inhibit, Prexasertib, SIK, S516, S296, RSK1, replication

Compound Identifiers

PubChem CID

46700756