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.
Product information
CAS Number: 1417630-95-5
Molecular Weight: 474.56
Formula: C25H30N8O2
Chemical Name: 2-[10-(2-methoxyethyl)-13-oxa-3,4,6,7,10-pentaazatricyclo[7.4.0.0²,⁶]trideca-1(9),2,4,7-tetraen-5-yl]-N-[(piperidin-4-yl)methyl]quinolin-8-amine
Smiles: COCCN1CCOC2C3=NN=C(C4=CC=C5C=CC=C(NCC6CCNCC6)C5=N4)N3N=CC1=2
InChiKey: BKDLGAKRAHVMNP-UHFFFAOYSA-N
InChi: InChI=1S/C25H30N8O2/c1-34-13-11-32-12-14-35-23-21(32)16-28-33-24(30-31-25(23)33)20-6-5-18-3-2-4-19(22(18)29-20)27-15-17-7-9-26-10-8-17/h2-6,16-17,26-27H,7-15H2,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. PIM1-IN-1 (2.5, 5, or 10 µM, 24 hours) induces apoptosis in SKMEL19 cells.
In Vivo:
PIM1-IN-1 shows cceptable clearance of 1.26 L/h/kg in BALB-C mice.
Products are for research use only. Not for human use.
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