PLX-4720

Name: PLX-4720
SKU: A10002
Price: 175 CNY
Rating: 5 (288 reviews)

目录号: A10002

Raf 抑制剂

PLX-4720 是一种强效且选择性的 B-RafV600E 抑制剂，其在无细胞试验中的 IC50 为 13 nM，对带有 Y340D 和 Y341D 突变的 c-Raf-1 同样具有强效，并且对 B-RafV600E 的选择性是野生型 B-Raf 的10倍。

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规格	价格	库存
5mg	¥175.00	现货
10mg	¥280.00	现货
25mg	¥490.00	现货
50mg	¥665.00	现货
100mg	¥840.00	现货
*10mM 1mL in DMSO**	¥245.00	现货
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Data Sheet

SDS

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生物活性

Discription

PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Targets

Target	Value

Cell Research

Cell Line	Type	Value	Description	References

In Vitro

Kinase Selectivity:
PLX-4720 exhibits high selectivity for the oncogenic B-Raf^V600E^ kinase, displaying >10 times selectivity against wild-type B-Raf and >100 times selectivity over other kinases, such as Frk, Src, Fak, FGFR, and Aurora A, with IC50 values ranging from 1.3 to 3.4 μM. ^[1]
ERK Phosphorylation Inhibition:
PLX-4720 significantly inhibits ERK phosphorylation in cell lines bearing the B-Raf^V600E^ mutation, with IC50 values ranging from 14 to 46 nM, while showing minimal effect on cells with wild-type B-Raf. ^[1]
Tumor Cell Growth Inhibition:
PLX-4720 potently inhibits the growth of tumor cell lines harboring the B-Raf^V600E^ oncogene. For example, it shows GI50 values of 0.31 μM in COLO205, 0.50 μM in A375, 1.5 μM in WM2664, and 1.7 μM in COLO829 cells. ^[1]
Induction of Apoptosis and Cell Cycle Arrest:
PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in B-Raf^V600E^ mutant cell lines, such as 1205Lu cells, but has no effect on B-Raf wild-type cells, such as C8161. ^[1]
PTEN Status and BIM Expression:
PLX-4720 treatment (10 μM) significantly increases BIM expression (>14-fold) in PTEN+ melanoma cells, whereas PTEN- cell lines exhibit only a 4-fold increase in BIM expression. This difference explains the resistance of PTEN- cells to PLX-4720-induced apoptosis. ^[2]

References

Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046. PMID: 18287029
Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71(7), 2750-2760. PMID: 21317224

产品信息

目录号	A10002
分子式	C17H14ClF2N3O3S
分子量	413.8
CAS号	918505-84-7
SMILES	CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)Cl)F
储存条件	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

溶解性数据

In vitro (25°C)	DMSO	81 mg/mL (195.73 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	2% DMSO+50% PEG 300+5% Tween 80+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	24.17 mL	120.83 mL	241.66 mL
0.5 mM	4.83 mL	24.17 mL	48.33 mL
1 mM	2.42 mL	12.08 mL	24.17 mL
5 mM	0.48 mL	2.42 mL	4.83 mL

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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