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[CAS NO. 1393465-84-3] PLX7904
| 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-18997 |
| Brand: | MCE |
| CAS: | 1393465-84-3 |
Overview
| MDL | MFCD29472265 |
|---|---|
| Molecular Weight | 512.53 |
| Molecular Formula | C24H22F2N6O3S |
| SMILES | O=S(NC1=CC=C(F)C(C(C2=CNC3=NC=C(C4=CN=C(C5CC5)N=C4)C=C32)=O)=C1F)(N(CC)C)=O |
3 Publications Citing Use of MCE
Summary
IC50 & Target
|
BRaf V600E 5 nM (IC 50 , in mutant RAS expressing cells) |
In Vitro
PLX7904 inhibits the in vitro growth of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 that expresses BRAF V600E with IC 50 values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, on a par with vemurafenib IC 50 values in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively) [1] . PLX7904 and PLX8394 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 and PLX8394 treatment at 1 μM concentration reduce colony formation and viability in parental cells to a similar level as PLX4720 [2] . PPLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells. PPLX7904 inhibits ERK1/2 in PLX470-resistant cell lines. PPLX7904 treatment promotes apoptosis and inhibits anchorage-independent growth of vemurafenib resistant cells [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 30 mg/mL ( 58.53 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9511 mL | 9.7555 mL | 19.5111 mL |
| 5 mM | 0.3902 mL | 1.9511 mL | 3.9022 mL |
| 10 mM | 0.1951 mL | 0.9756 mL | 1.9511 mL |
-
1.
References
- [1] Zhang C, et al. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature. 2015 Oct 22;526(7574):583-586.
- [2] Basile KJ, et al. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-84
- [3] Le K, et al. Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cells. Pigment Cell Melanoma Res. 2013 Jul;26(4):509-17
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