Trametinib DMSO solvate

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
500mg	$290	Check With Us
1g	$470	Check With Us
5g	$1185	Check With Us

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Cat #: V3642 CAS #: 1187431-43-1 Purity ≥ 98%

Description: Trametinib DMSO solvate is the solvated form of trametinib (trametinib: dimethyl sulfoxide=1:1) and a potent MEK inhibitor that specifically inhibits MEK1/2 with an IC50 value of about 2 nM.

References: Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with HWA486. Inflamm Res, 2012, 61(5), 445-454.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	693.09
Molecular Formula	C28H29FIN5O5S
CAS No.	1187431-43-1
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 10 mg/mLr
	Water: N/Ar
	Ethanol: N/A
SMILES Code	CC1=C2C(C(N(C3CC3)C(N2C4=CC(NC(C)=O)=CC=C4)=O)=O)=C(NC5=C(F)C=C(I)C=C5)N(C)C1=O.CS(C)=O
Synonyms	JTP-74057; JTP 74057; JTP74057; GSK-1120212 DMSO solvate;Trametinib; GSK-1120212;GSK1120212;GSK 1120212.

Protocol	In Vitro	In BRAF mutant SK-MEL-28 cells and KRAS mutant HCT116 cells, Trametinib (GSK1120212;JTP-74057) DMSO solvate causes dose-dependent inhibition of ERK1/2 phosphorylation as well as dose-dependent growth inhibition. In both SK-MEL-28 and HCT116 cells, Trametinib DMSO solvate inhibits 50% p-ERK1/2 at nearly equivalent concentrations (0.8 and 1.8 nM, respectively). However, as the slopes of the curves reflect, in SK-MEL-28 cells, Trametinib DMSO solvate inhibits 90% p-ERK1/2 at a lower concentration (3.4 nM) than in HCT116 (33.3 nM). Furthermore, in both cell lines, 50% growth inhibition is only achieved at concentrations Trametinib DMSO solvate that produces near complete ERK1/2 inhibition (85 and 90%, respectively).
Protocol	In Vivo	Trametinib (GSK1120212;JTP-74057) DMSO solvate is evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd×21). In this study, near complete tumor growth inhibition is observed at 5.0 and 2.5 mg/kg [92 and 87% tumor growth inhibition (TGI), respectively] and to a lesser degree at 0.5 and 0.1 mg/kg (62 and 58% TGI). Although 5 mg/kg is the maximally tolerated dose (MTD) in this study, 3 mg/kg is the typically observed MTD. Dose-dependent antitumor activity with Trametinib DMSO solvate treatment has been similarly reported for several other KRAS and BRAF mutant tumor models.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.4428 mL	7.2141 mL	14.4281 mL	28.8563 mL
5mM	0.2886 mL	1.4428 mL	2.8856 mL	5.7713 mL
10mM	0.1443 mL	0.7214 mL	1.4428 mL	2.8856 mL
20mM	0.0721 mL	0.3607 mL	0.7214 mL	1.4428 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.