AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. AZD6244 has potential to inhibit proliferation and induce apoptosis and differentiation, but the response varies between different xenografts.
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
AZD6244 purchased from AbMole
Sci Rep. 2021 Jun 14;11(1):12497.
Neuroprotective effect of selumetinib on acrolein-induced neurotoxicity
AZD6244 purchased from AbMole
Cell Reports. 2019 Feb 5;1518-1532.e9.
Pre-existing Functional Heterogeneity of Tumorigenic Compartment as the Origin of Chemoresistance in Pancreatic Tumors.
AZD6244 purchased from AbMole
Apoptosis. 2018 May 18.
Down-regulating IL-6/GP130 targets improved the anti-tumor effects of 5-fluorouracil in colon cancer.
AZD6244 purchased from AbMole
Cell Experiment | |
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Cell lines | HT-29, Malme-3M, MIAPaCa-2, SK-MEL-2, SK-MEL-28, BxPC3, BT-474, Zr-75-1, Malme-3 |
Preparation method | Cellular viability assays Cells plated in 96-well plates were incubated with multiple concentrations of compound for 3 days. The number of viable cells was determined using the CellTiter 96 Aqueous Nonradioactive Cell Proliferation Assay (Promega, Madison, WI). |
Concentrations | 0-50µM |
Incubation time | 3 days |
Animal Experiment | |
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Animal models | HT-29 and BxPC3 xenograft |
Formulation | 10% ethanol/10% cremophor EL/80% D5W |
Dosages | 10, 25, 50, or 100 mg/kg BID |
Administration | oral |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Molecular Weight | 457.68 |
Formula | C17H15BrClFN4O3 |
CAS Number | 606143-52-6 |
Purity | 100.0% |
Solubility | DMSO 30 mg/mL |
Storage | at -20°C |
Related MEK Products |
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Zapnometinib
Zapnometinib (PD0184264), an active metabolite of CI-1040, is an MEK inhibitor with an IC50 value of 5.7 nM. Zapnometinib has antiviral and antibacterial activity against influenza viruses. |
GW284543 (UNC10225170)
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RO5126766 (VS-6766)
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trans-Zeatin
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RO4987655
RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM. |
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