CRA-026440

Cat. No.: HY-19754: FAQs
Data Sheet Handling Instructions

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CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The K_i values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

CRA-026440 Chemical Structure

CAS No. : 847460-34-8

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Other In-stock Forms of CRA-026440:

Other Forms of CRA-026440:

CRA-026440 hydrochloride In-stock

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Description

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The K_i values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities^[1]. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

Ki: 4 nM (HDAC1), 14 nM (HDAC 2), 11 nM (HDAC3), 15 nM (HDAC6), 7 nM (HDAC8), 20 nM (HDAC10)^[1]

In Vitro

CRA-026440 has antiproliferative effect on HUVEC endothelial cells with a GI₅₀ value of 1.41 μM^[1].
CRA-026440 (0.1-10 μM; 18 hours) results in the accumulation of acetylated histone and acetylated tubulin, leading to an inhibition of tumor cell growth and the induction of apoptosis^[1].
CRA-026440 (0.1-10 μM; 5 days) inhibits ex vivo angiogenesis in a dose-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	HCT116 cells
Concentration:	0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time:	18 hours
Result:	Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1.

In Vivo

CRA-026440 (100 mg/kg; i.v.; daily; for three consecutive days) results in a statistically significant reduction in tumor growth in mice harboring HCT116 or U937 human tumor xenografts^[1].

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

Animal Model:	HCT-116 tumor-bearing nude mice^[1]
Dosage:	100 mg/kg
Administration:	i.v.; daily; for three consecutive days
Result:	Resulted in a statistically significant reduction in tumor growth.

Molecular Weight

420.46

Formula

C₂₃H₂₄N₄O₄

CAS No.

847460-34-8

SMILES

O=C(C(N1)=CC2=C1C=CC(OCCN(C)C)=C2)NCC#CC3=CC=C(C(NO)=O)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (237.83 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	2.3783 mL	11.8917 mL	23.7835 mL
5 mM	0.4757 mL	2.3783 mL	4.7567 mL
10 mM	0.2378 mL	1.1892 mL	2.3783 mL

View the Complete Stock Solution Preparation Table

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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 Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
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Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.3783 mL	11.8917 mL	23.7835 mL	59.4587 mL
	5 mM	0.4757 mL	2.3783 mL	4.7567 mL	11.8917 mL
	10 mM	0.2378 mL	1.1892 mL	2.3783 mL	5.9459 mL
	15 mM	0.1586 mL	0.7928 mL	1.5856 mL	3.9639 mL
	20 mM	0.1189 mL	0.5946 mL	1.1892 mL	2.9729 mL
	25 mM	0.0951 mL	0.4757 mL	0.9513 mL	2.3783 mL
	30 mM	0.0793 mL	0.3964 mL	0.7928 mL	1.9820 mL
	40 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4865 mL
	50 mM	0.0476 mL	0.2378 mL	0.4757 mL	1.1892 mL
	60 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9910 mL
	80 mM	0.0297 mL	0.1486 mL	0.2973 mL	0.7432 mL
	100 mM	0.0238 mL	0.1189 mL	0.2378 mL	0.5946 mL

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:

CRA-026440847460-34-8CRA026440CRA 026440Inhibitorinhibitorinhibit

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