CX-6258 hydrochloride hydrate

Cat. No.: HY-18095A Purity: 98.61%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CX-6258 hydrochloride hydrate 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 hydrochloride hydrate Chemical Structure

CAS No. : 1353858-99-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 164	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 164	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 192	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Other Forms of CX-6258 hydrochloride hydrate:

CX-6258 In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

CX-6258 hydrochloride hydrate 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]

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

516.42

Formula

C₂₆H₂₇Cl₂N₃O₄

CAS No.

1353858-99-7

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.[H]Cl.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (48.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 7.14 mg/mL (13.83 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9364 mL	9.6820 mL	19.3641 mL
5 mM	0.3873 mL	1.9364 mL	3.8728 mL
10 mM	0.1936 mL	0.9682 mL	1.9364 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 20% HP-β-CD in Saline
Solubility: 20 mg/mL (38.73 mM); Suspended solution; Need ultrasonic and warming and heat to 48°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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.61%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (257 KB) LCMS (265 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

H₂O / DMSO	1 mM	1.9364 mL	9.6820 mL	19.3641 mL	48.4102 mL
	5 mM	0.3873 mL	1.9364 mL	3.8728 mL	9.6820 mL
	10 mM	0.1936 mL	0.9682 mL	1.9364 mL	4.8410 mL
DMSO	15 mM	0.1291 mL	0.6455 mL	1.2909 mL	3.2273 mL
	20 mM	0.0968 mL	0.4841 mL	0.9682 mL	2.4205 mL
	25 mM	0.0775 mL	0.3873 mL	0.7746 mL	1.9364 mL
	30 mM	0.0645 mL	0.3227 mL	0.6455 mL	1.6137 mL
	40 mM	0.0484 mL	0.2421 mL	0.4841 mL	1.2103 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.