Art. -Nr.: HY-111552

PIM1-IN-1

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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.

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Reinheit: 99.83%
CAS. Nr.: 1417630-95-5
Formel: C₂₅H₃₀N₈O₂
Molecular Weight:474.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PIM1-IN-1 Chemical Structure

CAS. Nr.: 1417630-95-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PIM1

7 nM (IC₅₀)

PIM3

70 nM (IC₅₀)

PIM2

5530 nM (IC₅₀)

Alle Pim Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	GI₅₀	21.8 μM Compound: 42	Antiproliferative activity against human A375 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A375 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
A498	GI₅₀	8.98 μM Compound: 42	Antiproliferative activity against human A498 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A498 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
A549	GI₅₀	16.2 μM Compound: 42	Antiproliferative activity against human A549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
A673	GI₅₀	12.7 μM Compound: 42	Antiproliferative activity against human A673 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A673 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
ASPC1	GI₅₀	7.25 μM Compound: 42	Antiproliferative activity against human Aspc-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Aspc-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
BT-549	GI₅₀	20.4 μM Compound: 42	Antiproliferative activity against human BT549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human BT549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
BXPC-3	GI₅₀	9.21 μM Compound: 42	Antiproliferative activity against human BxPC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human BxPC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
CAKI-1	GI₅₀	22.1 μM Compound: 42	Antiproliferative activity against human CAKI-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human CAKI-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
COLO 205	GI₅₀	5.25 μM Compound: 42	Antiproliferative activity against human COLO205 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human COLO205 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
DU-145	GI₅₀	22.4 μM Compound: 42	Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HCT-116	GI₅₀	21.2 μM Compound: 42	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HL-60	GI₅₀	13.6 μM Compound: 42	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
JeKo-1	GI₅₀	7.3 μM Compound: 42	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
K562	GI₅₀	19.9 μM Compound: 42	Antiproliferative activity against human K562 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human K562 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
LNCaP	GI₅₀	18.6 μM Compound: 42	Antiproliferative activity against human LNCAP cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human LNCAP cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MCF7	GI₅₀	19.6 μM Compound: 42	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	GI₅₀	21.2 μM Compound: 42	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MIA PaCa-2	GI₅₀	17.4 μM Compound: 42	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MV4-11	GI₅₀	6.46 μM Compound: 42	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NAMALVA	GI₅₀	9.68 μM Compound: 42	Antiproliferative activity against human NAMALWA cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human NAMALWA cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H1299	EC₅₀	262 nM Compound: 42	Inhibition of PIM1 in human NCI-H1299 cells assessed as reduction in BAD phosphorylation at Ser-112 residue incubated for 4 hrs by ELISA Inhibition of PIM1 in human NCI-H1299 cells assessed as reduction in BAD phosphorylation at Ser-112 residue incubated for 4 hrs by ELISA	[PMID: 30802730]
NCI-H1650	GI₅₀	22.5 μM Compound: 42	Antiproliferative activity against human NCI-H1650 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human NCI-H1650 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H522	GI₅₀	9.7 μM Compound: 42	Antiproliferative activity against human NCI-H522 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human NCI-H522 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PANC-1	GI₅₀	25.4 μM Compound: 42	Antiproliferative activity against human PANC1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PANC1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PC-3	GI₅₀	17.1 μM Compound: 42	Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
Raji	GI₅₀	20 μM Compound: 42	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-BR-3	GI₅₀	21 μM Compound: 42	Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-ES1	GI₅₀	7.38 μM Compound: 42	Antiproliferative activity against human SK-ES-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-ES-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-MEL19	GI₅₀	1.48 μM Compound: 42	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	GI₅₀	23.5 μM Compound: 42	Antiproliferative activity against human SKOV3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SKOV3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SW480	GI₅₀	8.17 μM Compound: 42	Antiproliferative activity against human SW480 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SW-620	GI₅₀	8.73 μM Compound: 42	Antiproliferative activity against human SW620 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SW620 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T47D	GI₅₀	10.8 μM Compound: 42	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T84	GI₅₀	23.2 μM Compound: 42	Antiproliferative activity against human T84 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T84 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-251	GI₅₀	17.8 μM Compound: 42	Antiproliferative activity against human U251 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U251 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-87MG ATCC	GI₅₀	21.7 μM Compound: 42	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1417630-95-5
Appearance Solid
Molecular Weight 474.56
Formel C₂₅H₃₀N₈O₂
Color Light yellow to yellow
SMILES

COCCN1C2=C(C3=NN=C(C4=NC5=C(NCC6CCNCC6)C=CC=C5C=C4)N3N=C2)OCC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 45 mg/mL (94.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1072 mL

10.5361 mL

21.0722 mL

5 mM

0.4214 mL

2.1072 mL

4.2144 mL

10 mM

0.2107 mL

1.0536 mL

2.1072 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1072 mL	10.5361 mL	21.0722 mL	52.6804 mL
	5 mM	0.4214 mL	2.1072 mL	4.2144 mL	10.5361 mL
	10 mM	0.2107 mL	1.0536 mL	2.1072 mL	5.2680 mL
	15 mM	0.1405 mL	0.7024 mL	1.4048 mL	3.5120 mL
	20 mM	0.1054 mL	0.5268 mL	1.0536 mL	2.6340 mL
	25 mM	0.0843 mL	0.4214 mL	0.8429 mL	2.1072 mL
	30 mM	0.0702 mL	0.3512 mL	0.7024 mL	1.7560 mL
	40 mM	0.0527 mL	0.2634 mL	0.5268 mL	1.3170 mL
	50 mM	0.0421 mL	0.2107 mL	0.4214 mL	1.0536 mL
	60 mM	0.0351 mL	0.1756 mL	0.3512 mL	0.8780 mL
	80 mM	0.0263 mL	0.1317 mL	0.2634 mL	0.6585 mL

Keywords

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PIM1-IN-1

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Pim Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PIM1-IN-1

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Pim Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PIM1-IN-1 Related Classifications

Art. -Nr.: HY-111552