WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200313
CAS#: 869357-68-6
Description: AZD8330, also known as ARRY704 and ARRY424704, is an orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor AZD8330 specifically inhibits mitogen-activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers.
MedKoo Cat#: 200313
Name: AZD-8330
CAS#: 869357-68-6
Chemical Formula: C16H17FIN3O4
Exact Mass: 461.02478
Molecular Weight: 461.23
Elemental Analysis: C, 41.67; H, 3.72; F, 4.12; I, 27.51; N, 9.11; O, 13.88.
Synonym: AZD8330; AZD-8330; AZD 8330; ARRY424704; ARRY 424704; ARRY-424704; ARRY704; ARRY-704; ARRY 704.
IUPAC/Chemical Name: 2-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide.
InChi Key: RWEVIPRMPFNTLO-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H17FIN3O4/c1-9-7-11(15(23)20-25-6-5-22)14(21(2)16(9)24)19-13-4-3-10(18)8-12(13)17/h3-4,7-8,19,22H,5-6H2,1-2H3,(H,20,23)
SMILES Code: O=C(C(C=C1C)=C(NC2=CC=C(I)C=C2F)N(C)C1=O)NOCCO
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM. |
| In vitro activity: | With AZD8330 treatment, cell proliferation, and ERK1/2 pathway-associated Bcl-2, caspase-3, VEGF and p-ERK1/2 were assessed within cells with TRIM65 overexpression. As shown in Figure 4, TRIM65 overexpression significantly elevated cell proliferation as time went on, and induced higher levels of Bcl-2, VEGF and p-ERK1/2 while lower levels of caspse-3 when compared with control group, suggesting a progressive tumorigenesis of those two cells, yet, alone AZD8330 treatment on Jurkat and Raji cells presented an obviously opposite effect. However, with AZD8330 treatment on cells transfected with TRIM65 overexpression, TRIM65 overexpression-induced changes were significantly alleviated. These data showed that TRIM65 overexpression plus AZD8330 group remarkably inhibited cell viability, reduced Bcl-2, VEGF and p-ERK1/2 while enhanced cleaved-caspase 3 when compared with TRIM65 overexpression group (all P < 0.05). Reference: Cell Biol Int. 2018 Nov;42(11):1503-1510. https://pubmed.ncbi.nlm.nih.gov/30039885/ |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 74.0 | 160.44 | |
| DMSO:PBS (pH 7.2) (1:2) | 0.33 | 0.72 | |
| DMF | 30.0 | 65.04 | |
| Ethanol | 51.0 | 110.57 |
The following data is based on the product molecular weight 461.23 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Yang S, Yuan L, Wang Y, Zhu M, Wang J, Ke X. B7-H6 Promotes Cell Proliferation, Migration and Invasion of Non-Hodgkin Lymphoma via Ras/MEK/ERK Pathway Based on Quantitative Phosphoproteomics Data. Onco Targets Ther. 2020 Jun 18;13:5795-5805. doi: 10.2147/OTT.S257512. PMID: 32606790; PMCID: PMC7308182. 2. Wang J, Liang X, Yu T, Xu YL, Xu LH, Zhang XJ, Ma J, Wang YR, He SL. TRIM65 is a potential oncogenic protein via ERK1/2 on Jurkat and Raji cells: A therapeutic target in human lymphoma malignancies. Cell Biol Int. 2018 Nov;42(11):1503-1510. doi: 10.1002/cbin.11035. Epub 2018 Sep 11. PMID: 30039885. |
| In vitro protocol: | 1. Yang S, Yuan L, Wang Y, Zhu M, Wang J, Ke X. B7-H6 Promotes Cell Proliferation, Migration and Invasion of Non-Hodgkin Lymphoma via Ras/MEK/ERK Pathway Based on Quantitative Phosphoproteomics Data. Onco Targets Ther. 2020 Jun 18;13:5795-5805. doi: 10.2147/OTT.S257512. PMID: 32606790; PMCID: PMC7308182. 2. Wang J, Liang X, Yu T, Xu YL, Xu LH, Zhang XJ, Ma J, Wang YR, He SL. TRIM65 is a potential oncogenic protein via ERK1/2 on Jurkat and Raji cells: A therapeutic target in human lymphoma malignancies. Cell Biol Int. 2018 Nov;42(11):1503-1510. doi: 10.1002/cbin.11035. Epub 2018 Sep 11. PMID: 30039885. |
| In vivo protocol: | TBD |
AZD8330 is an orally active, selective MEK inhibitor with an IC50 of 7 nM. AZD8330 has potential antineoplastic activity. AZD8330 specifically inhibits mitogen- activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation.
