1417630-95-5

1417630-95-5 structure

Name: PIM1-IN-1
Chemical Name: PIM1-IN-1
CAS Number: 1417630-95-5
Molecular Formula: C₂₅H₃₀N₈O₂
Molecular Weight: 474.56
Catalog: Signaling Pathways JAK/STAT Signaling Pim
Create Date: 2019-03-30 16:02:34
Modify Date: 2024-01-10 09:11:34
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity[1].

Name	PIM1-IN-1

Description	PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> Pim
Target	PIM1:7 nM (IC50) PIM3:70 nM (IC50) PIM2:5530 nM (IC50)
In Vitro	PIM1-IN-1 (Compound 42) exhibits antiproliferative activity, with GI50 of 1.48 µM for melanoma cell line SKMEL-19. PIM1-IN-1 has significant synergistic effect combined with different antitumoral agents in different tumor cell lines[1]. PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells[1]. Apoptosis Analysis[1] Cell Line: SKMEL19 cells Concentration: 2.5, 5, or 10 µM Incubation Time: 24 hours Result: Regulated cell cycle, induced cell apopsis in SKMEL19 cells.
In Vivo	PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice[1].
References	[1]. Martínez-González S, et al. Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. Eur J Med Chem. 2019 Feb 19;168:87-109.

Molecular Formula	C₂₅H₃₀N₈O₂
Molecular Weight	474.56