[CAS NO. 1454682-72-4] LY3009120
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PRODUCTS SPECIFICATIONS [1454682-72-4]
Store
Catalog
SLK-S7842
Brand
Selleck
CAS
1454682-72-4
DESCRIPTION [1454682-72-4]
Overview
| MDL | MFCD28411374 |
|---|---|
| Molecular Weight | 424.51 |
| Molecular Formula | C23H29FN6O |
| SMILES | O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3557 mL | 11.7783 mL | 23.5566 mL |
| 5 mM | 0.4711 mL | 2.3557 mL | 4.7113 mL |
| 10 mM | 0.2356 mL | 1.1778 mL | 2.3557 mL |
| 50 mM | - | - | - |
Description
LY03009120 (DP-4978) is a potent pan- inhibitor with of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces . Phase 1.
Targets
In vitro
LY3009120 inhibits the cell growth of A375 and HCT116 cells with the IC50 of 9.2 and 220 μM, respectively. LY3009120 inhibits the tyrosine kinase KDR with the IC50 of 3.9 μM.
In vivo
In rats bearing BRAF V600E ST019VR PDX tumors, LY3009120 (15 or 30 mg/kg, p.o.) shows a dose-dependent tumor growth inhibition. In nude rats bearing A375 xenograft, single dose oral treatment with LY3009120 (3 to 50 mg/kg, p.o.) shows a dose dependent inhibition of phospho-ERK, with a dose for 50% inhibition of phospho-ERK (EC50) of 4.36 mg/kg, with plasma concentration to achieve 50% inhibition of phospho-ERK (EC50) of 68.9 ng/mL or 165 nM.
References
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