Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H19N7O2.CH4O3S.H2O |
| Molecular Weight | 479.51 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CS(O)(=O)=O.COC1=CC=CC(OCCCN)=C1C2=CC(NC3=CN=C(C=N3)C#N)=NN2
InChI
InChIKey=LCYWXOLNJNHLGN-UHFFFAOYSA-N
InChI=1S/C18H19N7O2.CH4O3S.H2O/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17;1-5(2,3)4;/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25);1H3,(H,2,3,4);1H2
LY2606368 (Prexasertib) is a small-molecule Chk-1 inhibitors invented by Array and being developed by Eli Lilly and Company. Lilly is responsible for all clinical development and commercialization activities. LY2606368 is advancing in Phase 2 clinical trials for cancer. Prexasertib preferentially binds to and inhibits CHK1 and, to a lesser extent, inhibits CHK2. Chk-1 is a protein kinase that regulates the tumor cell's response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, Chk-1 blocks cell cycle progression in order to allow for repair of damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting Chk-1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4630 |
0.9 nM [Ki] | ||
Target ID: CHEMBL2527 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
Sample Use Guides
105 mg/m2 IV once every 14 days of a 28 day cycle
Route of Administration:
Intravenous
In a functional assay, LY2606368 (PREXASERTIB) potently abrogated the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nmol/L. LY2606368 did inhibit DNA damage-induced CHK2 autophosphorylation with an IC50 of less than 31 nmol/L. 100 nmol/L LY2606368 did not inhibit PMA-stimulated RSK but instead weakly stimulated phosphorylation of S6 on serines 235/236. LY2606368 was broadly antiproliferative with IC50 values typically <50 nmol/L in the most sensitive cell lines with a minority of cell lines showing considerable resistance with IC50's >1,000 nmol/L
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FDA ORPHAN DRUG |
472015
Created by
admin on Sat Dec 16 10:32:21 GMT 2023 , Edited by admin on Sat Dec 16 10:32:21 GMT 2023
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46836099
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S4D3L195S4
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admin on Sat Dec 16 10:32:21 GMT 2023 , Edited by admin on Sat Dec 16 10:32:21 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD
