K882
K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C18H16N2O2
- Molecular Weight:292.33
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
PI3Kα |
XIAP |
JAK1 |
Stat-3 |
K882 (0.5-8 μM, 24-72 h) exhibits remarkable inhibitory activities on proliferation, migration and invasion in KRASG12C mutant NCI-H358 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI-H358
-
Concentration:0.5, 1, 2 and 4 μM
-
Incubation Time:24 h
-
Result:Blocked the NCI-H358 cell cycle in the G2/M phase.
-
Cell Line:NCI-H358
-
Concentration:1, 2, 4, 8 μM
-
Incubation Time:24 h
-
Result:Increased the rate of apoptotic cells concentration-dependently.
Inhibited the expressions of two apoptosis inhibitory proteins (XIAP and Survivin).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:NCI-H358 xenograft tumor mice model[1]
-
Dosage:25, 50 and 100 mg/kg,
-
Administration:Intraperitoneal injection (i.p.), once a day, 31 days
-
Result:Decreased tumor volume.
Showed the tumor inhibitory rates of 42.48 % (25 mg/kg), 49.72% (50 mg/kg) and 60.39 % (100 mg/kg).
Abrogated the phosphorylation at Y416 of Src.
Did not exhibit any apparent damage in the vital organs.
Chemical Information
-
Molecular Weight 292.33
-
Formula C18H16N2O2
-
SMILES
COC1=CC(/C=C/C2=NC=NC3=CC=CC=C23)=C(OC)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)