Pim-1 kinase inhibitor 8

Name: Pim-1 kinase inhibitor 8
Brand: MedChemExpress
SKU: HY-162006
Rating: 4.5 (1 reviews)

Cat. No.: HY-162006 Purity: 99.90%: Data Sheet
COA

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Pim-1 kinase inhibitor 8 is a potent PIM-1 inhibitor with an IC₅₀ value of 14.3 nM. Pim-1 kinase inhibitor 8 impedes cell proliferation and migration through PIM-1 inhibition and the induction of both apoptosis and autophagy. Pim-1 kinase inhibitor 8 inhibits solid tumor growth in Solid Ehrlich Carcinoma (SEC)-bearing mice. Pim-1 kinase inhibitor 8 can be used for breast and liver cancer research.

For research use only. We do not sell to patients.

Pim-1 kinase inhibitor 8 Chemical Structure

CAS No. : 916038-47-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

Pim-1 kinase inhibitor 8 (compound 12) (0.01-100 μM, 48 h) exhibits potent cytotoxicity against MCF-7 and HepG2 cell lines with IC₅₀ values of 0.51 μM and 5.27 μM, respectively, while showing much lower potency in normal MCF-10A cells (IC₅₀ = 52.85 μM)^[1].
Pim-1 kinase inhibitor 8 (1.62 μM, 48 h) triggers considerable apoptotic and autophagic cell death in MCF-7 cells, accompanied by cell cycle arrest at the S-phase, and shows significant inhibition of cell migration (71.8 % wound closure vs. 95.6 % in the control)^[1].
Pim-1 kinase inhibitor 8 binds strongly to the PIM-1 active site (-17.38 kcal/mol) by forming a key hydrogen bond with Lys67 and multiple hydrophobic interactions^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	MCF-7 cells
Concentration:	1.62 μM
Incubation Time:	48 h
Result:	Increased the proportion of cells in the S-phase to 36.02 %, compared to 29.12 % in the control. Reduced the proportion of cells in the G2/M phase from 16.05 % (control) to 7.56 %.

Apoptosis Analysis^[1]

Cell Line:	MCF-7 cells
Concentration:	1.62 μM
Incubation Time:	48 h
Result:	Increased total apoptosis by 33.43 % (23.18 % for early apoptosis and 10.25 % for late apoptosis) compared to the untreated control group (0.64 %). Increased apoptosis by 52.2-fold.

Cell Cytotoxicity Assay^[1]

Cell Line:	MCF-7 and HepG2 cells
Concentration:	0.01, 0.1, 1, 10, and 100 μM
Incubation Time:	48 h
Result:	Inhibited the growth of MCF-7 and HepG2 cells by 84.20 % and 85.13 %, respectively, at 100 μM.

Cell Autophagy Assay^[1]

Cell Line:	MCF-7 cells
Concentration:	1.62 μM
Incubation Time:	48 h
Result:	Caused considerable autophagic cell death, markedly increasing the autophagic cell population to 87.6 × 10³ cells compared to 32.8 × 10³ in the control.

In Vivo

Pim-1 kinase inhibitor 8 (5 mg/kg, i.p., daily for 24 days) demonstrates significant tumor inhibition in solid tumors in SEC-bearing mice^[1].

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

Animal Model:	Adult female Swiss albino mice (18-23 g) subcutaneously injected with SEC cells^[1]
Dosage:	5 mg/kg
Administration:	i.p., daily for 24 days
Result:	Decreased tumor weight from 198.5 mg in control to 72.8 mg. Reduced tumor volume from 274.8 mm³ in the untreated control to 159.2 mm³. Greatly decreased tumor proliferation by 42.1 %.

Molecular Weight

275.30

Formula

C₁₄H₁₇N₃O₃

CAS No.

916038-47-6

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(OCC(N2CCOCC2)=O)N=C(C)C=C1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (454.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6324 mL	18.1620 mL	36.3240 mL
5 mM	0.7265 mL	3.6324 mL	7.2648 mL
10 mM	0.3632 mL	1.8162 mL	3.6324 mL

View the Complete Stock Solution Preparation Table

* 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.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.90%

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Data Sheet (277 KB) SDS (251 KB)

COA (248 KB) HNMR (236 KB) LCMS (84 KB)

Handling Instructions (2659 KB)

References

[1]. Shaban SM, et al. Design and Synthesis of Novel Pyridine-Based Compounds as Potential PIM-1 Kinase Inhibitors, Apoptosis, and Autophagy Inducers Targeting MCF-7 Cell Lines: In Vitro and In Vivo Studies. ACS Omega. 2023 Nov 27;8(49):46922-46933. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.6324 mL	18.1620 mL	36.3240 mL	90.8100 mL
	5 mM	0.7265 mL	3.6324 mL	7.2648 mL	18.1620 mL
	10 mM	0.3632 mL	1.8162 mL	3.6324 mL	9.0810 mL
	15 mM	0.2422 mL	1.2108 mL	2.4216 mL	6.0540 mL
	20 mM	0.1816 mL	0.9081 mL	1.8162 mL	4.5405 mL
	25 mM	0.1453 mL	0.7265 mL	1.4530 mL	3.6324 mL
	30 mM	0.1211 mL	0.6054 mL	1.2108 mL	3.0270 mL
	40 mM	0.0908 mL	0.4541 mL	0.9081 mL	2.2703 mL
	50 mM	0.0726 mL	0.3632 mL	0.7265 mL	1.8162 mL
	60 mM	0.0605 mL	0.3027 mL	0.6054 mL	1.5135 mL
	80 mM	0.0454 mL	0.2270 mL	0.4541 mL	1.1351 mL
	100 mM	0.0363 mL	0.1816 mL	0.3632 mL	0.9081 mL