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AB141343

AZD6244, MEK1/2 inhibitor

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MW 457.7 Da, Purity >99%. Potent, selective, non-ATP competitive MEK1/2 inhibitor (IC50 MEK1 = 14 nM). Also inhibits ERK1/2 phosphorylation.

View Alternative Names

AAK1_HUMAN, AIS, ANDR_HUMAN, AP2 associated kinase 1, AP2-associated protein kinase 1, AR, AR8, Adaptor-associated kinase 1, Androgen nuclear receptor variant 2, Androgen receptor, Androgen receptor (dihydrotestosterone receptor, testicular feminization, spinal and bulbar muscular atrophy, Kennedy disease), Atherosclerosis, susceptibility to, included, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, BIKe, BMP-2-inducible protein kinase, BMP2 inducible kinase, BMP2K, BMP2K_HUMAN, Bike kinase, CFC syndrome, CFC4, CK II, CK II alpha', CK2A2, CSK22_HUMAN, Cardiofaciocutaneous syndrome, Casein kinase 2 alpha prime polypeptide, Casein kinase II alpha' chain, Casein kinase II subunit alpha', Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, DHTR, DKFZp434K0614, DKFZp434P0116, DKFZp686F03202, DKFZp686K16132, DKFZp686N23123, Dihydro testosterone receptor, Dihydrotestosterone receptor (DHTR), Dual specificity mitogen-activated protein kinase kinase 1, Dual specificity mitogen-activated protein kinase kinase 2, EGFR_HUMAN, ER, ER-alpha, ER-beta, ERBB, ERBB1, ERK activator kinase 1, ERK activator kinase 2, ER[a], ER[b], ESR, ESR B, ESR BETA, ESR1_HUMAN, ESRA, ESTR B, Epidermal growth factor receptor, Epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog), Epidermal growth factor receptor (erythroblastic leukemia viral (v erb b) oncogene homolog avian), Era, Erb, Erb2, Errp, Estr, Estra, Estradiol Receptor alpha, Estradiol Receptor beta, Estradiol receptor, Estrogen Receptor 1, Estrogen Receptor 2, Estrogen receptor, Estrogen receptor 1 (alpha), Estrogen receptor 2 (ER beta), Estrogen receptor 2 ER beta, Estrogen receptor alpha, Estrogen receptor beta 4, Estrogen resistance, included, FLJ23712, FLJ25931, FLJ26075, FLJ31060, FLJ42882, FLJ43934, FLJ45252, HDL cholesterol, augmented response of, to hormone replacement, included, HER1, HRIHFB2017, HUMARA, HYSP1, IMD42, KD, KIAA1048, Kennedy disease (KD), MAP kinase kinase 1, MAP kinase kinase 2, MAP kinase/Erk kinase 1, MAP2K1, MAP2K2, MAPK / ERK kinase 2, MAPK/ERK kinase 1, MAPKK 1, MAPKK 2, MEK 1, MEK 2, MEKK 1, MGC129539, MGC138170, MGC164568, MGC164570, MKK 1, MKK 2, MP2K1_HUMAN, MP2K2_HUMAN, Microtubule associated protein kinase kinase 2, Mitogen Activated Protein Kinase Kinase 1, Mitogen activated protein kinase kinase 2, Mitogen activated protein kinase kinase 2 p45, Myocardial infarction, susceptibility to, included, NISBD2, NR1F3, NR3A1, NR3A2, NR3C4, Nuclear receptor ROR-gamma, Nuclear receptor RZR-gamma, Nuclear receptor subfamily 1 group F member 3, Nuclear receptor subfamily 3 group A member 1, Nuclear receptor subfamily 3 group A member 2, Nuclear receptor subfamily 3 group C member 4, Nuclear receptor subfamily 3 group C member 4 (NR3C4), OTTHUMP00000017718, OTTHUMP00000017719, OTTHUMP00000165826, OTTHUMP00000165827, Oncogen ERBB, PIG61, PRKMK 1, PRKMK 2, Protein kinase mitogen activated kinase 1 (MAP kinase kinase 1), Proto-oncogene c-ErbB-1, RAR related orphan nuclear receptor variant 2, RAR related orphan receptor C, isoform a, RAR related orphan receptor gamma, RAR-related orphan receptor C, RNESTROR, RORG_HUMAN, RZR GAMMA, RZRG, Receptor tyrosine-protein kinase ErbB-1, Retinoic acid binding receptor gamma, Retinoid-related orphan receptor-gamma, Rorc, SA7, SBMA, SMAX1, Species antigen 7, Spinal and bulbar muscular atrophy, Spinal and bulbar muscular atrophy (SBMA), TFM, TOR, Testicular Feminization (TFM), Urogastrone, Wa5, androgen receptor splice variant 4b, erb-b2 receptor tyrosine kinase 1, mENA, protein kinase mitogen-activated kinase 1, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2

Key facts

CAS number

606143-52-6

Purity

>99%

Form

Solid

form

Molecular weight

457.7 Da

Molecular formula

C<sub>1</sub><sub>7</sub>H<sub>1</sub><sub>5</sub>BrClFN<sub>4</sub>O<sub>3</sub>

PubChem

10127622

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 4 mM

Biochemical name

Selumetinib

Biological description

Potent, selective, non-ATP competitive MEK1/2 inhibitor (IC50 MEK1 = 14 nM). Also inhibits ERK1/2 phosphorylation.

Canonical smiles

CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

InChi

InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)

InChiKey

CYOHGALHFOKKQC-UHFFFAOYSA-N

IUPAC Name

6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Handling instructions

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Toxic, refer to SDS for further information.

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Estrogen Receptor (ER) MEK1 EGFR MEK2 Androgen Receptor (AR) CSNK2A2 ROR gamma BMP2K and AAK1 are various proteins playing significant mechanical roles in cellular processes. The Estrogen Receptor also known as ERα or ESR1 has a mass of approximately 66 kDa and is abundantly expressed in breast tissue liver and ovaries. MEK1 and MEK2 both MAP2K proteins interact with the ERK/MAPK signaling pathway and are found in various tissues. EGFR another notable target is usually expressed on epithelial cells and has a mass around 170 kDa. The Androgen Receptor with a mass of 110 kDa appears in high levels in male reproductive tissues. CSNK2A2 (also called CK2 alpha' subunit) ROR gamma BMP2K and AAK1 have distinct cellular locations but contribute to signaling and regulation within cells.
Biological function summary

These targets perform critical roles in maintaining homeostasis and facilitating signal transduction within cells. Estrogen Receptor mediates estrogen signaling influencing transcription and cell proliferation. MEK1 and MEK2 act as kinases in the MAPK/ERK pathway essential for cell division and differentiation. EGFR is an important player in cell survival and proliferation and is part of a receptor tyrosine kinase complex. The Androgen Receptor regulates the expression of genes linked to male traits and reproduction occasionally forming complexes with co-regulators. CSNK2A2 aids in phosphorylation processes while ROR gamma BMP2K and AAK1 contribute to immune response and intracellular transport regulation.

Pathways

These proteins integrate into various important signaling networks. The Estrogen Receptor and Androgen Receptor are important in steroid hormone signaling pathways affecting gene expression and cellular activities. MEK1/2 linked with the MAPK/ERK pathway involves in response mechanisms to growth factors and hormones engaging with proteins like RAF and ERK. EGFR initiates numerous downstream signaling cascades including PI3K/AKT and JAK/STAT pathways influencing oncogenesis and survival. CSNK2A2 ROR gamma BMP2K and AAK1 align within pathways related to cell cycle regulation and immune signaling.

These targets are implicated in conditions such as cancer and metabolic diseases. Estrogen Receptor is notably connected to breast cancer interacting with proteins like HER2 which can alter treatment responses. Dysregulation of EGFR associates with several cancers including lung and colorectal cancer influenced by interplay with KRAS and BRAF proteins. Abnormal activity of MEK1/2 also relates to malignant cell transformation bearing connections to ERK. The Androgen Receptor has links to prostate cancer with interactions affecting diagnosis and therapy. Proteins CSNK2A2 ROR gamma BMP2K and AAK1 further involve in diverse disorders emphasizing their roles in cellular pathology.

Product protocols

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