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[CAS NO. 945614-12-0] Pexmetinib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16782 |
| Brand: | MCE |
| CAS: | 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 |
1 Publications Citing Use of MCE
Summary
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
DMSO : ≥ 125 mg/mL ( 224.57 mM )
* "≥" means soluble, but saturation unknown.
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 |
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