Tunlametinib

SKU: orb3027324

Description

Tunlametinib is a highly selective, orally bioavailable small molecule inhibitor of MEK1 and MEK2 kinases with a reported IC50 value of 1.9 nM for MEK1. Tunlametinib exerts its antitumor effects by blocking the oncogenic RAS-RAF-MEK-ERK signaling pathway, thereby inducing tumor cell cycle arrest and promoting apoptosis, Tunlametinib demonstrates strong inhibitory activity against various RAS/RAF-mutant cancer cells such as those harboring BRAF V600E or KRAS G12C mutations, shows synergistic effects in combination with BRAF/KRASG12C/SHP2 inhibitors and Docetaxel, and is used in targeted therapy for RAS/RAF-driven cancers including melanoma, colorectal cancer, and non-small cell lung cancer (NSCLC).

Research Area

Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1801756-06-8
MW	491.25
Purity	98.72%
Formula	C₁₆H₁₂F₂IN₃O₃S
SMILES	O=C(NOCCO)C1=CC=2SC=NC2C(F)=C1NC3=CC=C(I)C=C3F
Target	Ras,MEK,Kras
Solubility	10% DMSO+40% PEG300+5% Tween-80+45% Saline:5 mg/mL (10.18 mM);DMSO:80 mg/mL (162.85 mM)

Bioactivity

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Target IC50	COLO 205 cells:0.94 nM\|HT-291 cells:10.07 nM\|HL-60 cells:0.67 nM\|A375 cells:0.86 nM\|Colo-829 cells:3.46 nM\|A549 cells:59.89 nM
In Vivo	Methods: Tunlametinib (1, 3, 6 mg/kg, oral, once daily for 21 days) was used to treat female BALB/c nude mice, NU/NU mice, or Nod-Scid mice bearing A375 (BRAF V600E mutant melanoma), COLO 205 (BRAF V600E mutant colon cancer), and Calu-6 (KRAS Q61K mutant lung cancer) tumors, and the tumor growth in vivo was observed. Results: Tunlametinib inhibited tumor growth in the above mice in a concentration-dependent manner. Read more...
In Vitro	Methods: A375 cells were treated with tunlametinib (1-9 nM, 48 h) to evaluate the effects on the cell cycle. Results: Tunlametinib increased the proportion of A375 cells in the G0/G1 phase in a dose-dependent manner and induced cell cycle arrest. Methods: Tunlametinib was used to treat BRAF/KRAS mutant cell lines: A375, Colo-829, HL-60 melanoma cells, COLO 205, HT-29 colon cancer cells, Calu-6, A549 lung cancer cells, and cell viability was determined by MTS assay. Results: The IC50 values of tunlametinib in the above cells were 0.86 nM, 3.46 nM, 0.67 nM, 0.94 nM, 10.07 nM, and 59.89 nM. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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HL085, HL-085, Tunlametinib

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Gene Symbol

Ras,MEK,Kras

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Tunlametinib (orb3027324)

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Tunlametinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Quick Database Links

Documents Download

Request a Document

Protocol Information

Tunlametinib (orb3027324)

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