AZD0424

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AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.

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AZD0424 Chemical Structure

CAS No. : 692054-06-1

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Description

AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity^[1]. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells^[2].

IC₅₀ & Target

Src/Abl kinase inhibitor (SrcK-I), apoptosis^[1]

In Vitro

AZD0424 (1-5 μM; 24-48 hours) is emerged to be the more effective of the three tested inhibitors (AZM559756, AZD0530 and AZD0424), inducing the highest levels of apoptosis with the lowest concentrations in lymphoma cells^[2].
AZD0424 (5 μM; 48 hours) leads to increased G0/G1 cell cycle arrest in DOHH-2 and WSU-NHL cells, whereas the cell cycle progression of the nonsensitive cell lines Raji and Jurkat remains unaffected^[2].

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

Apoptosis Analysis^[2]

Cell Line:	DOHH-2, WSU-NHL, Raji, Jurkat, Karpas-299 and HUT78 cells
Concentration:	1 μM; 2 μM; 3 μM; 4 μM; 5 μM;
Incubation Time:	24 hours, 48 hours
Result:	Induced apoptosis in lymphoma cells.

Cell Cycle Analysis^[2]

Cell Line:	DOHH-2, WSU-NHL, Raji and Jurkat cells
Concentration:	1 μM; 2 μM; 3 μM; 4 μM; 5 μM;
Incubation Time:	48 hours
Result:	Increased G0/G1 cell cycle arrest in DOHH-2 and WSU-NHL cells.

Clinical Trial

Molecular Weight

528.99

Formula

C₂₅H₂₉ClN₆O₅

CAS No.

692054-06-1

SMILES

CC(N1CCN(CCOC2=CC3=NC=NC(NC4=C(OCO5)C5=NC=C4Cl)=C3C(OC(C)C)=C2)CC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Woodcock VK, et al. A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424. Br J Cancer. 2018 Mar 20;118(6):770-776. [Content Brief]

[2]. Nowak D, et al. Src kinase inhibitors induce apoptosis and mediate cell cycle arrest in lymphoma cells. Anticancer Drugs. 2007 Oct;18(9):981-95. [Content Brief]

AZD0424 Related Classifications

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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:

AZD0424692054-06-1AZD 0424AZD-0424SrcBcr-AblApoptosisInhibitorinhibitorinhibit

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