AZD0424 is a selective Src/Abl kinase inhibitor that can be taken orally and has anti-tumor activity. AZD0424 can cause apoptosis and cell cycle arrest in lymphoma cells.

Physicochemical Properties

Molecular Formula	C25H29CLN6O5
Molecular Weight	528.987964391708
Exact Mass	528.188
CAS #	692054-06-1
PubChem CID	9893171
Appearance	Typically exists as solid at room temperature
LogP	3.2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	10
Rotatable Bond Count	8
Heavy Atom Count	37
Complexity	759
Defined Atom Stereocenter Count	0
InChi Key	MVWATCATLSSVBH-UHFFFAOYSA-N
InChi Code	InChI=1S/C25H29ClN6O5/c1-15(2)37-20-11-17(34-9-8-31-4-6-32(7-5-31)16(3)33)10-19-21(20)24(29-13-28-19)30-22-18(26)12-27-25-23(22)35-14-36-25/h10-13,15H,4-9,14H2,1-3H3,(H,27,28,29,30)
Chemical Name	1-[4-[2-[4-[(6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-5-propan-2-yloxyquinazolin-7-yl]oxyethyl]piperazin-1-yl]ethanone
Synonyms	AZD0424 AZD-0424 AZD 0424
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Of the three inhibitors studied (AZM559756, AZD0530, and AZD0424), AZD0424 (1–5 μM; 24-48 hours) was shown to be the most powerful, generating the highest amounts of apoptosis in lymphoma cells at the lowest concentration[2]. In DOHH-2 and WSU-NHL cells, AZD0424 (5 μM; 48 hours) results in increased G0/G1 cell cycle arrest; however, cell cycle progression is unaffected in the non-sensitive cell lines Raji and Jurkat [2].
Cell Assay	Apoptosis analysis[2] Cell Types: DOHH-2, WSU-NHL, Raji, Jurkat, Karpas-299 and HUT78 Cell Tested Concentrations: 1 μM; 2μM; 3μM; 4μM; 5μM; Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results:Induces lymphoma cell apoptosis. Cell cycle analysis[2] Cell Types: DOHH-2, WSU-NHL, Raji and Jurkat Cell Tested Concentrations: 1 μM; 2μM; 3μM; 4μM; 5μM; Incubation Duration: 48 hrs (hours) Experimental Results: In DOHH-2 and WSU-NHL cells Increased G0/G1 cell cycle arrest.
References	[1]. 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. [2]. Src kinase inhibitors induce apoptosis and mediate cell cycle arrest in lymphoma cells. Anticancer Drugs. 2007 Oct;18(9):981-95.
Additional Infomation	AZD0424 has been used in trials studying the treatment of Advanced Solid Tumours. Src/Abl Kinase Inhibitor AZD0424 is an orally bioavailable small molecule tyrosine kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Upon oral administration, AZD0424 selectively inhibits both Src and Abl kinase activity which may result in the inhibition of tumor growth in susceptible tumor cells. Src and Abl kinases are upregulated in certain tumor cells and play important roles in tumor cell proliferation and metastasis.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.8904 mL	9.4520 mL	18.9039 mL
	5 mM	0.3781 mL	1.8904 mL	3.7808 mL
	10 mM	0.1890 mL	0.9452 mL	1.8904 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.