CRT0066854 hydrochloride

Name: CRT0066854 hydrochloride
Brand: MedChemExpress
SKU: HY-18713A
Rating: 4.5 (1 reviews)

Cat. No.: HY-18713A Purity: 99.29%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively.

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

CRT0066854 hydrochloride Chemical Structure

CAS No. : 2250019-91-9

Size	Price	Stock	Quantity
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of CRT0066854 hydrochloride:

CRT0066854 Get quote

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•Related Screening Libraries:

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View All PKC Isoform Specific Products:

View All Isoforms

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

View All ROCK Isoform Specific Products:

View All Isoforms

ROCK ROCK1 ROCK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PKCζ

639 nM (IC₅₀)

ROCKII

620 nM (IC₅₀)

In Vitro

CRT0066854 hydrochloride displaces a crucial Asn-Phe-Asp motif that is part of the adenosine-binding pocket and engages an acidic patch used by arginine-rich PKC substrates^[1].
CRT0066854 hydrochloride (0.2-1.2 μM; 6 days) is able to restore polarized morphogenesis in the dysplastic H-Ras spheroids, and the maximal proportion of spheroids with PSALs is at the lower dose of 1.2 μM^[1].

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

Molecular Weight

452.01

Formula

C₂₄H₂₆ClN₅S

CAS No.

2250019-91-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

N[C@H](CNC1=NC(C2=CC=NC=C2)=NC3=C1C(CCCC4)=C4S3)CC5=CC=CC=C5.[H]Cl

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 : 100 mg/mL (221.23 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	2.2123 mL	11.0617 mL	22.1234 mL
5 mM	0.4425 mL	2.2123 mL	4.4247 mL
10 mM	0.2212 mL	1.1062 mL	2.2123 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.

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: ≥ 5 mg/mL (11.06 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.06 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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: 99.29%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (258 KB) HNMR (466 KB) RP-HPLC (257 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. Kjær S, et al. Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes. Biochem J. 2013 Apr 15;451(2):329-42. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2123 mL	11.0617 mL	22.1234 mL	55.3085 mL
	5 mM	0.4425 mL	2.2123 mL	4.4247 mL	11.0617 mL
	10 mM	0.2212 mL	1.1062 mL	2.2123 mL	5.5309 mL
	15 mM	0.1475 mL	0.7374 mL	1.4749 mL	3.6872 mL
	20 mM	0.1106 mL	0.5531 mL	1.1062 mL	2.7654 mL
	25 mM	0.0885 mL	0.4425 mL	0.8849 mL	2.2123 mL
	30 mM	0.0737 mL	0.3687 mL	0.7374 mL	1.8436 mL
	40 mM	0.0553 mL	0.2765 mL	0.5531 mL	1.3827 mL
	50 mM	0.0442 mL	0.2212 mL	0.4425 mL	1.1062 mL
	60 mM	0.0369 mL	0.1844 mL	0.3687 mL	0.9218 mL
	80 mM	0.0277 mL	0.1383 mL	0.2765 mL	0.6914 mL
	100 mM	0.0221 mL	0.1106 mL	0.2212 mL	0.5531 mL