CX-6258

Cat. No.: HY-18095 Purity: 98.71%: FAQs
Data Sheet SDS COA Handling Instructions

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CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC₅₀s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.

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

CX-6258 Chemical Structure

CAS No. : 1202916-90-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 91	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 91	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 135	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 266	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
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Other Forms of CX-6258:

CX-6258 hydrochloride hydrate In-stock
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PIM1 PIM2 PIM3

Biological Activity
Purity & Documentation
References
Customer Review

Description

CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC₅₀s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively^[1].

IC₅₀ & Target

IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	> 10 μM Compound: 13	Inhibition of Flt3 phosphorylation at Y591 in human MV411 cells after 2 hrs by Western blot analysis Inhibition of Flt3 phosphorylation at Y591 in human MV411 cells after 2 hrs by Western blot analysis	[PMID: 24900437]
PC-3	IC₅₀	452 nM Compound: 13	Cytotoxicity against human PC3 cells assessed as viability after 96 hrs Cytotoxicity against human PC3 cells assessed as viability after 96 hrs	[PMID: 24900437]

In Vitro

CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively^[1].
CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells^[2].
CX-6258 treatment results in a significant reduction in NKX3.1 half-life^[2].

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

Western Blot Analysis^[1]

Cell Line:	MV-4-11 human AML cells
Concentration:	0.1 μM, 1 μM, 10 μM
Incubation Time:	2 hours
Result:	Caused dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.

In Vivo

CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models^[1].

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

Animal Model:	Nude mice, MV-4-11 xenograft models^[1]
Dosage:	50 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; over a period of 21 days
Result:	Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.

Molecular Weight

461.94

Formula

C₂₆H₂₄ClN₃O₃

CAS No.

1202916-90-2

Appearance

Solid

Color

Yellow to orange

SMILES

O=C1NC2=CC=C(Cl)C=C2/C1=C\C3=CC=C(C4=CC=CC(C(N5CCCN(C)CC5)=O)=C4)O3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (108.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1648 mL	10.8239 mL	21.6478 mL
5 mM	0.4330 mL	2.1648 mL	4.3296 mL
10 mM	0.2165 mL	1.0824 mL	2.1648 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 20 mg/mL (43.30 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.71%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (255 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139

[2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1648 mL	10.8239 mL	21.6478 mL	54.1196 mL
	5 mM	0.4330 mL	2.1648 mL	4.3296 mL	10.8239 mL
	10 mM	0.2165 mL	1.0824 mL	2.1648 mL	5.4120 mL
	15 mM	0.1443 mL	0.7216 mL	1.4432 mL	3.6080 mL
	20 mM	0.1082 mL	0.5412 mL	1.0824 mL	2.7060 mL
	25 mM	0.0866 mL	0.4330 mL	0.8659 mL	2.1648 mL
	30 mM	0.0722 mL	0.3608 mL	0.7216 mL	1.8040 mL
	40 mM	0.0541 mL	0.2706 mL	0.5412 mL	1.3530 mL
	50 mM	0.0433 mL	0.2165 mL	0.4330 mL	1.0824 mL
	60 mM	0.0361 mL	0.1804 mL	0.3608 mL	0.9020 mL
	80 mM	0.0271 mL	0.1353 mL	0.2706 mL	0.6765 mL
	100 mM	0.0216 mL	0.1082 mL	0.2165 mL	0.5412 mL

CX-6258 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CX-62581202916-90-2CX6258CX 6258PimPim kinasesBad4E-BP1Inhibitorinhibitorinhibit

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