[CAS NO. 945614-12-0] Pexmetinib

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PRODUCTS SPECIFICATIONS [945614-12-0]

Catalog

HY-16782

Brand

MCE

CAS

945614-12-0

DESCRIPTION [945614-12-0]

Overview

MDL	MFCD28502055
Molecular Weight	556.63
Molecular Formula	C31H33FN6O3
SMILES	O=C(NCC1=CC(F)=CC=C1OC2=CC3=C(N(CCO)N=C3)C=C2)NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Mol Hum Reprod. 2021 Feb 24;gaab014.

Summary

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC ₅₀ s of 1 nM, 35 nM and 26 nM for Tie-2 , p38α and p38β , respectively, and can be used in the research of acute myeloid leukemia.

IC50 & Target

IC50: 1 nM (Tie-2), 35 nM (p38α), 26 nM (p38β) ^[1]

In Vitro

Pexmetinib is a Tie-2 and p38 MAPK dual inhibitor, with IC ₅₀ s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively. Pexmetinib also shows IC ₅₀ s of 4 nM (Abl), 10 nM (Arg), 28 nM (FGFR1), 47 nM (Flt1), 42 nM (Flt4), 41 nM (Fyn), 26 nM (Hck), 25 nM (Lyn), and 26 nM (MINK), respectively. Pexmetinib (0.5, 1 μM) blocks leukemic cell proliferation and stimulates hematopoietic activity in myelodysplastic syndromes ^[1] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04074967	Jason J. Luke, MD\|Array BioPharma\|University of Pittsburgh	Renal Cell Carcinoma\|Melanoma\|Solid Tumor\|Non-small Cell Lung Cancer\|Head and Neck Squamous Cell Carcinoma	June 11, 2020	Phase 1\|Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 125 mg/mL ( 224.57 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7965 mL	8.9826 mL	17.9653 mL
5 mM	0.3593 mL	1.7965 mL	3.5931 mL
10 mM	0.1797 mL	0.8983 mL	1.7965 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Bachegowda L, et al. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res. 2016 Aug 15;76(16):4841-4849.