PROTAC SOS1 degrader-2

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PROTAC SOS1 degrader-2 是一种有效的PROTAC SOS1降解剂。 PROTAC SOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTAC SOS1degrader-2 在体内显著抑制肿瘤生长。

生物活性

PROTACSOS1 degrader-2 is a potentPROTACSOS1degrader.PROTACSOS1 degrader-2 decreases the expression ofpERKand RAS-GTP level in a dose-dependent manner.PROTACSOS1 degrader-2 significantly inhibits the tumor growth in vivo^[1].

IC₅₀& Target^[1]

K-RAS

体外研究
(In Vitro)

PROTAC SOS1 degrader-2 (compound 9d) (0.1, 1 μM) shows a potent SOSI degradation activity with an SOS1 protein degradation of 56.2 and 92.5% at 0.1 and 1 μM in NCI-H358 cells, respectively^[1].
PROTAC SOS1 degrader-2 (24 h) degrades SOS1 in a dose- and time-dependent manner in NCI-H358 cells^[1].
PROTAC SOS1 degrader-2 (9.8-2500 nM; 24 h) does not induce SOS2 and KRAS degradation in NCI-H358 cells^[1].
PROTAC SOS1 degrader-2 (7.8-2000 nM; 24 h) decreases the expression of pERK and RAS-GTP level in NCI-H358 cells in a dose-dependent manner^[1].

Western Blot Analysis^[1]

Cell Line:	NCI-H358 cells
Concentration:	7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time:	24 h
Result:	Showed a potent degradation activity with an EC₅₀of 98.4 nM in NCI-H358 cells.

RT-PCR^[1]

Cell Line:	NCI-H358 cells
Concentration:	1 μM
Incubation Time:	24, 48, 72 h
Result:	Showed the SOS2 mRNA level remained constant during the incubation period.

Cell Proliferation Assay^[1]

Cell Line:	NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells
Concentration:	0-10000 nM
Incubation Time:	7 days
Result:	Inhibited the cell growth with IC₅₀s of 0.525, 0.218, 0.307, 0.115, 0.199, 0.232 μM (EC₅₀s of 0.098, 0.255, 0.119, 0.104, 0.125, 0.022 μM)for NCI-H358, MIA PaCa2, AsPC-1, SK-LU-1, SW620, A549 cells, respectively.

体内研究
(In Vivo)

PROTAC SOS1 degrader-2 (10, 20 mg/kg; i.p., daily for 21 days ) significantly inhibits the tumor growth in vivo with a good safety profile^[1].

Animal Model:	BALB/c nude mice (NCI-H358 tumor xenografts)^[1]
Dosage:	10, 20 mg/kg
Administration:	I.p.; daily, 21 days
Result:	Significantly inhibited the tumor growth in vivo with a good safety profile.

分子量

1051.79

Formula

C₅₇H₇₆ClFN₁₀O₄S

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.