CST905
CST905 is a potent BRAF-V600E PROTAC degrader with a DC50 of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma.
(Pink: BRAF-V600E ligand (HY-41747); Blue: VHL ligand (HY-125845); Black: linker (HY-78378)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3094183-98-6
- 分子式: C51H58F2N10O7S2
- 分子量:1025.20
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
BRafV600E 18 nM (DC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL-28 | GI50 |
61 nM
|
Exerts inhibitory effects on cell proliferation and reduces cell viability in human malignant melanoma SK-MEL-28 cells.
Exerts inhibitory effects on cell proliferation and reduces cell viability in human malignant melanoma SK-MEL-28 cells.
|
35814929 |
体外実験
CST905 (0.1-10 μM; 4-24 h) exerts effects of degrading BRAF-V600E protein (IC50 = 18 nM) and inhibiting ERK1/2 phosphorylation (IC50 = 31 nM) in human malignant melanoma SK-MEL-28 cells[1].
CST905 (up to 10 μM; 120 h) exerts inhibitory effects on cell proliferation and reduces cell viability in human malignant melanoma SK-MEL-28 cells (GI50 = 61 nM)[1].
CST905 (0.1-10 μM; 4-24 h) does not induce abnormal activation of p-ERK1/2 or p-MEK1/2, nor does it affect the expression of wild-type BRAF protein or the level of p-ERK1/2 in human neuroblastoma SK-N-AS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:SK-MEL-28 cell line and SK-N-AS cell line
-
Concentration:0.1, 1, 10 μM
-
Incubation Time:4 h
-
Result:Decreased the intracellular expression level of the mutant target protein and effectively down-regulated the phosphorylation activation of downstream signaling molecules.
Did not cause paradoxical hyperphosphorylation and activation of downstream key kinase signals in the mutant cells, avoiding undesirable paradoxical activation.
-
Cell Line:SK-MEL-28 cell line
-
Concentration:1.56 nM, 3.13 nM, 6.25 nM, 12.5 nM, 25 nM, 50 nM, 100 nM, 1 μM, 10 μM
-
Incubation Time:4 h
-
Result:Induced degradation of the mutant target protein in a concentration-dependent manner, achieved maximal degradation at 50 nM, and concentration-dependently suppressed the phosphorylation activation of downstream signaling molecules.
-
Cell Line:SK-MEL-28 cell line
-
Concentration:0.59 nM, 1.77 nM, 5.33 nM, 16.0 nM, 48.0 nM, 144.0 nM, 432.0 nM, 1296.0 nM, 3888.0 nM, 10 μM
-
Incubation Time:120 h
-
Result:Inhibited the in vitro proliferation and viability of tumor cells in a concentration-dependent manner.
-
Cell Line:SK-N-AS cell line
-
Concentration:0.1, 1, 10 μM (4 h treatment) and 10 μM (24 h treatment)
-
Incubation Time:4 h, 24 h
-
Result:Did not alter the normal expression abundance of the wild-type target protein and did not disturb basal downstream phosphorylation levels.
化学情報
-
CAS 番号 3094183-98-6
-
分子量 1025.20
-
分子式 C51H58F2N10O7S2
-
SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(C4=CN=C(NC=C5C(C6=C(F)C=CC(NS(=O)(N(CC)C)=O)=C6F)=O)C5=C4)C=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CST905 関連分類
HY-175435 関連分類
Powered by Bioz