PIM1-IN-1

Modify Date: 2024-01-10 09:11:34

PIM1-IN-1 Structure
PIM1-IN-1 structure
Common Name PIM1-IN-1
CAS Number 1417630-95-5 Molecular Weight 474.56
Density N/A Boiling Point N/A
Molecular Formula C25H30N8O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PIM1-IN-1


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].

 Names

Name PIM1-IN-1

 PIM1-IN-1 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C25H30N8O2
Molecular Weight 474.56
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: PIM1-IN-1
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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