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Products are for research use only. Not for human use. We do not sell to patients.
(IC-83; LY 2603618; LY-2603618)
LY2603618 Chemical Structure
|Product name: LY2603618|
|Cat. No.: HY-14720|
LY2603618(IC-83) is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to enter clinical cancer trials.
IC50 Value: 7 nM
in vitro: LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preclinical data involving LY2603618 has not been published until now.
in vivo: In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed.
|M.Wt||436.3||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≤ 29.5 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.2920 mL||11.4600 mL||22.9200 mL|
|5 mM||0.4584 mL||2.2920 mL||4.5840 mL|
|10 mM||0.2292 mL||1.1460 mL||2.2920 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|LY2603618||Eli Lilly & Co||Cancer||30-JUN-11||31-DEC-12||Phase 1||15-FEB-13|
|Eli Lilly & Co||Non-small-cell lung cancer||30-NOV-09||30-APR-13||Phase 2||12-JUN-13|
|Eli Lilly & Co||Solid tumor||31-MAY-11||31-DEC-14||Phase 1||11-NOV-13|
|Eli Lilly & Co||Solid tumor||28-FEB-11||30-NOV-13||Phase 2||01-NOV-13|
|Eli Lilly & Co||Pancreas tumor||31-MAR-09||31-MAY-13||Phase 2||11-NOV-13|
|Eli Lilly & Co||Metastatic non small cell lung cancer||28-FEB-11||30-NOV-13||Phase 2||01-NOV-13|
. Weiss GJ, Donehower RC, Iyengar T, Ramanathan RK, Lewandowski K, Westin E, Hurt K, Hynes SM, Anthony SP, McKane S.Phase I dose-escalation study to examine the safety and tolerability of LY2603618, a checkpoint 1 kinase inhibitor, administered 1 day after pemetrexed 500 mg/m(2) every 21 days in patients with cancer.Invest New Drugs. 2012 Apr 11.
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CCT244747 is potent, highly selective, orally active, ATP competitive CHK1 inhibitor with IC50 of 29-170nM.
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