303727-31-3

Name	L-779450
Synonyms	L-779450 2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol 2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]phenol 2-Chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-iMidazol-4-yl)phenol Phenol, 2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-iMidazol-5-yl]- 4-(4-Chloro-3-hydroxyphenyl)-2-phenyl-5-(4-pyridyl)-1H-iMidazole 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole 4-(4-Chloro-3-hydroxyphenyl)-2-phenyl-5-(pyridin-4-yl)-1H-iMidazole
CAS	303727-31-3

Molecular Formula	C20H14ClN3O
Molar Mass	347.8
Density	1.335±0.06 g/cm3(Predicted)
Boling Point	579.8±50.0 °C(Predicted)
pKa	8.09±0.10(Predicted)
Storage Condition	Sealed in dry,2-8°C
In vitro study	L-779450 (L-779,450) shows a high degree of specificity towards Raf. The only other tested kinase inhibited is p38MAPK, which has a kinase domain structurally related to Raf. L-779450 inhibits anchorage-independent growth of human tumor lines at doses ranging from 0.3 to 2 μM. The effects of L-779450 (L-779,450) on TRAIL sensitivity are investigated here in melanoma cell lines with high TRAIL sensitivity (A-375 and SK-Mel-147), moderate sensitivity (Mel-HO, SK-Mel-13, and SK-Mel-28), and permanent resistance (MeWo, Mel-2a, and SK-Mel-103), as well as in TRAIL-selected cell lines with acquired resistance (A-375-TS and Mel-HO-TS). Despite only moderate direct effects of L-779450 on apoptosis, it strongly enhances TRAIL-induced apoptosis in sensitive melanoma cells and overrules TRAIL resistance in Mel-2a, SK-Mel-103, A-375-TS, and Mel-HO-TS. At 24 hours, 16-35% apoptosis induction is obtained.

Last Update：2024-01-02 23:10:35

biological activity	L-779450 is a potent, low nanomolar B- raf inhibitor with an IC50 of 10 nM, kd was 2.4 nM.
Target	Value
B-Raf (Cell-free assay)	2.4 nM(Kd) 10 nM

Last Update：2024-04-09 20:48:19

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303727-31-3

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