Selumetinib (AZD6244)
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MedKoo CAT#: 200300

CAS#: 606143-52-6

Description: Selumetinib, also known as AZD6244, is an orally bioavailable small molecule with potential antineoplastic activity. Selumetinib inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, and so may inhibit cellular proliferation in MEK-overexpressing tumor cells.


Chemical Structure

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Selumetinib (AZD6244)
CAS# 606143-52-6

Theoretical Analysis

MedKoo Cat#: 200300
Name: Selumetinib (AZD6244)
CAS#: 606143-52-6
Chemical Formula: C17H15BrClFN4O3
Exact Mass: 456.00001
Molecular Weight: 457.68
Elemental Analysis: C, 44.61; H, 3.30; Br, 17.46; Cl, 7.75; F, 4.15; N, 12.24; O, 10.49

Size Price Shipping out time Quantity
200mg USD 150 Same day
500mg USD 250 Same day
1g USD 450 Same day
2g USD 650 Same day
5g USD 1150 Same day
10g USD 1950 Same day
20g USD 2950 Same day
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

Selumetinib, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: AZD6244; AZD-6244; AZD 6244; ARRY142886; ARRY 142886; ARRY-142886; ARRY886; ARRY-886; ARRY 886 ; selumetinib.

IUPAC/Chemical Name: 6-[(4-bromo-2-chlorophenyl)amino]-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide

InChi Key: CYOHGALHFOKKQC-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(C1=C(NC2=CC=C(Br)C=C2Cl)C(F)=C3C(N(C)C=N3)=C1)NOCCO

Appearance:
white 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

Preparing Stock Solutions

The following data is based on the product molecular weight 457.68 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: El-Hoss J, Kolind M, Jackson MT, Deo N, Mikulec K, McDonald MM, Little CB, Little DG, Schindeler A. Modulation of endochondral ossification by MEK inhibitors PD0325901 and AZD6244 (Selumetinib). Bone. 2013 Nov 20. doi:pii: S8756-3282(13)00474-2. 10.1016/j.bone.2013.11.013. [Epub ahead of print] PubMed PMID: 24269278.

2: Jain N, Curran E, Iyengar NM, Diaz-Flores E, Kunnavakkam R, Popplewell L, Kirschbaum MH, Karrison TG, Erba HP, Green M, Poire X, Koval G, Shannon K, Reddy PL, Joseph L, Atallah EL, Dy P, Thomas SP, Smith S, Doyle A, Stadler WM, Larson R, Stock W, Odenike OM. Phase II Study Of The Oral MEK Inhibitor Selumetinib In Advanced Acute Myeloid Leukemia (AML): A University Of Chicago Phase II Consortium Trial. Clin Cancer Res. 2013 Oct 31. [Epub ahead of print] PubMed PMID: 24178622.

3: Bid HK, Kibler A, Phelps DA, Manap S, Xiao L, Lin J, Capper D, Oswald D, Geier B, Dewire M, Smith PD, Kurmasheva RT, Mo X, Fernandez S, Houghton PJ. Development, Characterization, and Reversal of Acquired Resistance to the MEK1 Inhibitor Selumetinib (AZD6244) in an In Vivo Model of Childhood Astrocytoma. Clin Cancer Res. 2013 Nov 22. [Epub ahead of print] PubMed PMID: 24132923.

4: Paolo M, Assunta S, Antonio R, Claudia SP, Anna BM, Clorinda S, Francesca C, Fortunato C, Cesare G. Selumetinib in advanced non small cell lung cancer (NSCLC) harbouring KRAS mutation: endless clinical challenge to KRAS-mutant NSCLC. Rev Recent Clin Trials. 2013 Jun;8(2):93-100. PubMed PMID: 24063423.

5: Beloueche-Babari M, Jamin Y, Arunan V, Walker-Samuel S, Revill M, Smith PD, Halliday J, Waterton JC, Barjat H, Workman P, Leach MO, Robinson SP. Acute tumour response to the MEK1/2 inhibitor selumetinib (AZD6244, ARRY-142886) evaluated by non-invasive diffusion-weighted MRI. Br J Cancer. 2013 Sep 17;109(6):1562-9. doi: 10.1038/bjc.2013.456. Epub 2013 Aug 13. PubMed PMID: 23942066; PubMed Central PMCID: PMC3776979.

6: Selumetinib shows promise in metastatic uveal melanoma. Cancer Discov. 2013 Jul;3(7):OF8. doi: 10.1158/2159-8290.CD-NB2013-086. Epub 2013 Jun 6. PubMed PMID: 23847383.

7: Selumetinib increases the efficacy of first-line dacarbazine. Cancer Discov. 2013 Jul;3(7):OF16. doi: 10.1158/2159-8290.CD-RW2013-129. Epub 2013 Jun 13. PubMed PMID: 23847359.

8: Spreafico A, Tentler JJ, Pitts TM, Tan AC, Gregory MA, Arcaroli JJ, Klauck PJ, McManus MC, Hansen RJ, Kim J, Micel LN, Selby HM, Newton TP, McPhillips KL, Gustafson DL, Degregori JV, Messersmith WA, Winn RA, Eckhardt SG. Rational combination of a MEK inhibitor, selumetinib, and the Wnt/calcium pathway modulator, cyclosporin A, in preclinical models of colorectal cancer. Clin Cancer Res. 2013 Aug 1;19(15):4149-62. doi: 10.1158/1078-0432.CCR-12-3140. Epub 2013 Jun 11. PubMed PMID: 23757356.

9: Robert C, Dummer R, Gutzmer R, Lorigan P, Kim KB, Nyakas M, Arance A, Liszkay G, Schadendorf D, Cantarini M, Spencer S, Middleton MR. Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: a phase 2 double-blind randomised study. Lancet Oncol. 2013 Jul;14(8):733-40. doi: 10.1016/S1470-2045(13)70237-7. Epub 2013 Jun 2. PubMed PMID: 23735514.

10: Sabnis GJ, Kazi A, Golubeva O, Shah P, Brodie A. Effect of selumetinib on the growth of anastrozole-resistant tumors. Breast Cancer Res Treat. 2013 Apr;138(3):699-708. doi: 10.1007/s10549-013-2474-5. Epub 2013 Mar 19. PubMed PMID: 23508762.  



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