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LY2603618

HY-14720

(IC-83; LY 2603618; LY-2603618)

LY2603618

LY2603618 Chemical Structure

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.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $140 In-stock
50 mg $440 In-stock
100 mg $700 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €97 In-stock
5 mg €88 In-stock
10 mg €137 In-stock
50 mg €431 In-stock
100 mg €686 In-stock
200 mg Get quote
500 mg Get quote

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Inquiry Information
Product name: LY2603618
Cat. No.: HY-14720

LY2603618 Data Sheet

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    Purity: 99.99%

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Biological Activity of LY2603618

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
Target: Chk1
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.

Chemical Information

M.Wt 436.3 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C18H22BrN5O3
CAS No 911222-45-2
Solvent & Solubility

DMSO ≥20mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

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

Clinical Information of LY2603618

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

References on LY2603618

Inhibitor Kit

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