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Tunlametinib

Name: Tunlametinib
Brand: TargetMol
SKU: T39220
Price: 66 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T39220Cas No. 1801756-06-8

Alias HL-085, HL085

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).

Tunlametinib

🥰Excellent

Purity: 98.72%

Catalog No. T39220Alias HL-085, HL085Cas No. 1801756-06-8

Pack Size	Price	Availability
1 mg	$66	In Stock
5 mg	$158	In Stock
10 mg	$248	In Stock
25 mg	$397	In Stock
1 mL x 10 mM (in DMSO)	$173	In Stock

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Purity:98.72%

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COA LCMS HNMR

Product Introduction

Bioactivity

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).
Targets&IC50	HT-291 cells:10.07 nM, Colo-829 cells:3.46 nM, A375 cells:0.86 nM, COLO 205 cells:0.94 nM, HL-60 cells:0.67 nM, A549 cells:59.89 nM
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. [1]
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. [1]
Synonyms	HL-085, HL085

Chemical Properties

Molecular Weight	491.25
Formula	C₁₆H₁₂F₂IN₃O₃S
Cas No.	1801756-06-8
Smiles	O=C(NOCCO)C1=CC=2SC=NC2C(F)=C1NC3=CC=C(I)C=C3F
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (162.85 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0356 mL	10.1781 mL	20.3562 mL	101.7812 mL
5 mM	0.4071 mL	2.0356 mL	4.0712 mL	20.3562 mL
10 mM	0.2036 mL	1.0178 mL	2.0356 mL	10.1781 mL
20 mM	0.1018 mL	0.5089 mL	1.0178 mL	5.0891 mL
50 mM	0.0407 mL	0.2036 mL	0.4071 mL	2.0356 mL
100 mM	0.0204 mL	0.1018 mL	0.2036 mL	1.0178 mL

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