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PROTAC EGFR degrader 3

PROTAC EGFR degrader 3 是一种有效的 PROTAC EGFR 降解剂。PROTAC EGFR degrader 3 对 H1975 和 HCC827 细胞具有优异的细胞活性和高选择性。PROTAC EGFR degrader 3 表明溶酶体参与了 EGFR 突变体的降解过程。

PROTAC EGFR degrader 3 Chemical Structure

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生物活性

PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation^[1].

体外研究
(In Vitro)

PROTAC EGFR degrader 3 (compound CP17) shows anti-proliferative activity of PROTACs with IC₅₀s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFR^L858/T790M), HCC827 (EGFR^del19), A431 (EGFR^WT) cells, respectively^[1].
PROTAC EGFR degrader 3 (0, 10, 100, 1000, 10000 nM) exhibits poor cellular activity with IC₅₀ of 481 nM, 669 nM for Ba/F3 (EGFR^{del19/T790M/C797S}) and Ba/F3 (EGFR^{L858/T790M/C797S}) cells, respectively^[1].
PROTAC EGFR degrader 3 (0-10000 nM) suppresses the proliferation of the PC9 (EGFR^{del19/T790M/C797S}) and H1975 (EGFR^{L858/T790M/C797S}) cells, respectively^[1].
PROTAC EGFR degrader 3 (30 nM; 0-72 h) decreases the expression level of EGFR^L858/T790M after 8h, and degradation rate maximizes after 48 h^[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24, 48 h) induces the degradation of EGFR^L858/T790M and EGFR^del19 with DC₅₀s of 1.56 nM and 0.49 nM, respectively^[1].
PROTAC EGFR degrader 3 (100, 1000 nM; 24 h) shows selective against mutant EGFR in the H1975 and HCC827 cells^[1].
PROTAC EGFR degrader 3 (0.3, 1, 3, 10, 100, 300 nM; 24 h) effectively blocks EGFR singnal transduction, leading to cell proliferation inhibition^[1].
PROTAC EGFR degrader 3 (30 nM) induces EGFR mutant degradation, and the lysosome is involved in the degradation process^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	H1975 (EGFR^L858/T790M), HCC827 (EGFR^del19), A431 (EGFR^WT) cells
Concentration:
Incubation Time:	72 h
Result:	Exhibited anti-proliferative activity of PROTACs with IC₅₀s of 32 nM, 1.60 nM, >10000nM for H1975 (EGFR^L858/T790M), HCC827 (EGFR^del19), A431 (EGFR^WT) cells, respectively.

Western Blot Analysis^[1]

Cell Line:	H1975, HCC827 cells
Concentration:	0.3, 1, 3, 10, 30 nM
Incubation Time:	24 h
Result:	Remarkably decreased the phosphorylated EGFR, ERK, AKT in the H1975 and HCC827 cells.

分子量

1092.40

Formula

C₆₀H₇₇N₁₃O₅S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Zhao HY, et al. Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. J Med Chem. 2022; 65(6):4709-4726.

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