2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. MEK ERK Apoptosis p38 MAPK CDK PARP
  4. RO5068760

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.

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RO5068760

RO5068760 Chemical Structure

CAS No. : 947182-25-4

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RO5068760 Related Antibodies

Top Publications Citing Use of Products

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4

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ERK ERK1 ERK2 ERK5 ERK8

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research[1].

IC50 & Target[1]

MEK1

0.025 μM (IC50)

MEK2

 

In Vitro

RO5068760 significantly inhibits MAPK pathway activity as evidenced by the dose-dependent inhibition of both ERK and MEK phosphorylation (p-ERK and p-MEK) in many human cancer cell lines, such as LOX, HT-29, H460, and MIA PaCa-2 cells[1].
RO5068760 specifically inhibits cell growth in cancer cell lines with activating pathway gene mutations (B-Raf or KRas), and the representative IC50/IC90 values are 0.018/0.72 μM in LOX (B-RafV600E), 0.11/0.56 μM in HT-29 (B-RafV600E), 0.30/3.08 μM in H460 (KRasG12C), and 1.25/5.11 μM in MIA PaCa-2 (KRasQ61K) cancer cells[1].
RO5068760 (0-10 μM, 24 h) downregulates CDK4/cyclin D1 and upregulates p27 and cleaved PARP in responsive cancer cells (HT-29 and LOX), indicating that it induces G1 cell cycle arrest and subsequently leads to apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RO5068760 Related Antibodies

Western Blot Analysis[1]

Cell Line: HT-29 and LOX cells
Concentration: 0, 2, and 10 μM
Incubation Time: 24 h
Result: Decreased CDK4 and cyclin D1 levels in a dose dependent manner.
Increased p27 and cleaved PARP levels in HT-29 and LOX cells.
In Vivo

RO5068760 (6.25-500 mg/kg, p.o., b.i.d. or q.d. or weekly for approximately 3 to 4 weeks) exhibits dose-dependent antitumor activity in corresponding human tumor xenograft models in mice with aberrant MAPK pathway activation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice subcutaneously implanted with human cancer cells (LOX and HT-29 (both B-Raf V600E mutant), MIA PaCa-2 (KRAS G12C mutation) and H460 (KRAS Q61H mutation))[1]
Dosage: 6.25, 12.5, 25, 50, 100, 200 and 500 mg/kg
Administration: p.o., b.i.d. or q.d. or weekly for approximately 3 to 4 weeks
Result: Showed significant tumor growth inhibition (TGI > 65%) in all models when administered once or twice daily.
Exhibited partial (PR) or complete regression (CR) at doses as low as 12.5 mg/kg (b.i.d.) in the LOX melanoma model harboring B-RafV600E mutation.
Resulted in PR or CR in four of four tumor models tested at a dose of 100 mg/kg twice daily.
Exhibited antitumor activity in the LOX melanoma model even at 500 mg/kg once weekly with three PRs and five CRs compared with vehicle controls.
In K-Ras mutant tumors, twice-daily dosing yielded better efficacy than once-daily or weekly regimens at equivalent total doses.
Showed superior in vivo efficacy in B-RafV600E xenografts (LOX and HT-29) compared with K-Ras mutant xenografts (H460 and MIA PaCa-2).
In the MIA PaCa-2 and H460 xenograft models, Cmax levels in plasma reached or exceeded the EC90 of p-ERK suppression, whereas in the LOX and HT-29 models, maximal plasma levels required for a similar degree of efficacy were significantly lower.
Molecular Weight

647.43

Formula

C28H27FIN3O6
CAS No.
SMILES

C[C@@H](C1=CC=CC=C1)[C@H](N2C([C@@H](C3=CC=C(C=C3)OC[C@H](O)CO)NC2=O)=O)C(NC4=C(C=C(C=C4)I)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RO5068760 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RO5068760947182-25-4RO 5068760RO-5068760MEKERKApoptosisp38 MAPKCDKPARPMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesCyclin dependent kinasepoly ADP ribose polymerasenon-ATP-competitiveMEK1/2MAPKmelanomacolorectal cancerNSCLCpancreatic cancerLOXHT-29H460MIA PaCa-2Inhibitorinhibitorinhibit

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