Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C23H28FN7O |
Molecular Weight | 437.5131 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN[C@H]1CCN(C1)C(=O)C2=CC=C(NC3=NC=C(F)C(=N3)C4=CN=C(C)N4C(C)C)C=C2
InChI
InChIKey=NTSDIJMNXYJJNG-SFHVURJKSA-N
InChI=1S/C23H28FN7O/c1-14(2)31-15(3)26-12-20(31)21-19(24)11-27-23(29-21)28-17-7-5-16(6-8-17)22(32)30-10-9-18(13-30)25-4/h5-8,11-12,14,18,25H,9-10,13H2,1-4H3,(H,27,28,29)/t18-/m0/s1
Molecular Formula | C23H28FN7O |
Molecular Weight | 437.5131 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/18996007
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18996007
AZD-5597 is potent imidazole pyrimidine amide CDK inhibitor with in vitro anti-proliferative effects against a range of cancer cell lines. AZD-5597 exhibited excellent aqueous solubility, photostability, hydrolytic stability, plasma stability and the lack of CYP inhibition. In nude mice implanted subcutaneously with SW620 human colon adenocarcinoma cells, AZD-5597 (15 mg/kg, dosed intermittently for 3 weeks, ip) inhibited tumor volume by 55%. The overall profile of AZD-5597 indicated that it was suitable for further development as an iv agent.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL308 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18996007 |
2.0 nM [IC50] | ||
Target ID: CHEMBL301 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18996007 |
2.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18996007
Nude mice were treated intermittently (Monday, Wednesday, Friday) for 3 weeks at 15 mg/kg
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18996007
The colorectal cancer cell lines LoVo were used for activity evaluation. Cells were plated in 96-well plates with medium containing 0.125% FBS for 24 h and then treated with medium containing 10% FBS and the test compound (AZD-5597) at various concentrations, and incubated for 48 h. Compounds activity was evaluated by Bromodeoxyuridine assay.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 07:59:42 GMT 2023
by
admin
on
Sat Dec 16 07:59:42 GMT 2023
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Record UNII |
N7855W19GY
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Record Status |
Validated (UNII)
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Record Version |
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