PROTAC BRAF-V600E degrader-1

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CAS NO:

2417296-84-3

PROTAC BRAF-V600E degrader-1 是一种有效的PROTAC BRAF-V600E降解剂，对 BRAF 和 BRAF-V600E 的K_d分别为 2.4 nM 和 2 nM。PROTAC BRAF-V600E degrader-1 通过泛素-蛋白酶体系统 (UPS) 降解 BRAF-V600E。PROTAC BRAF-V600E degrader-1 可抑制黑色素瘤细胞的生长。

生物活性

PROTACBRAF-V600E degrader-1 is a potentPROTACBRAF-V600Edegrader withK_dvalue of 2.4 nM and 2 nM forBRAFand BRAF-V600E, respectively.PROTACBRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS).PROTACBRAF-V600E degrader-1 can inhibit melanoma cell growth^[1].

IC₅₀& Target^[1]

BRAF-V600E

2 nM (Kd)

Braf

2.4 nM (Kd)

体外研究
(In Vitro)

PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell viability of A375 and HT-29^[1].
PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h or 0-24 h) inhibits p-ERK and BRAF-V600E protein in A375 cells^[1].

Cell Viability Assay^[1]

Cell Line:	A375 and HT-29
Concentration:	1 nM-10 μM
Incubation Time:	72 h
Result:	Inhibited the cell viability of A375 and HT-29 with IC₅₀s of 46.5 nM and 51 nM.

Western Blot Analysis^[1]

Cell Line:	A375
Concentration:	1, 4, 12, 37, 111, 333 and 1000 nM
Incubation Time:	16 h or 0-24 h
Result:	Induced the reduction in the phosphorylation of ERK. Inhibited p-ERK and BRAF-V600E in a dose- and time-dependent manner.

分子量

1001.07

性状

Solid

Formula

C₄₈H₅₄F₂N₁₀O₁₀S

CAS 号

2417296-84-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month