1. PROTAC Autophagy Immunology/Inflammation Apoptosis Cell Cycle/DNA Damage
  2. PROTACs FKBP
  3. dTAGV-1

dTAGV-1 是一种有效的和选择性的 FKBP12F36V 标记蛋白 PROTAC 降解剂。dTAGV-1 可以在体内诱导 FKBP12F36V-Nluc 降解。(Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A))

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dTAGV-1

dTAGV-1 Chemical Structure

CAS No. : 2451573-86-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

dTAGV-1 is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 can induce degradation of FKBP12F36V-Nluc in vivo. (Pink: Target Protein Ligand (HY-114420); Black: Linker (HY-W012001); Blue: VHL Ligand (HY-112078); VHL Ligan+Linker (HY-173628A))[1].

体外研究
(In Vitro)

dTAGV-1 (0.1 nM-10 μM; 24 小时) 诱导 FKBP12F36V-Nluc 强效降解,但对 293FT 细胞中的 FKBP12WT-Nluc 没有影响[1]
dTAGV-1 (125-2000 nM; 24 小时) 与 THAL-SNS-032 共同处理会导致 LACZ-FKBP12F36VCDK9[1] 均显著降解。
dTAGV-1 (500 nM; 1-24 小时) 导致 KRASG12V 和 pERK1/2 快速降解[1]
dTAGV-1 (50-5000 nM; 24 小时) 能够促进尤文氏肉瘤中的 EWS/FLI 降解[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

dTAGV-1 (35 mg/kg;腹腔注射,每日一次,共 4 天) 可诱导小鼠 FKBP12F36V-Nluc 降解[1]
dTAGV-1 (2-10 mg/kg;腹腔注射) 在小鼠中表现出半衰期(T1/2=3.64 和 4.4 h)、Cmax (595 和 2123 ng/mL)和高暴露量(AUCinf =3136 和 18517 h ng/mL)[1]
dTAGV-1 (2 mg/kg;静脉注射) 表现出半衰期(T1/2=3.02 h)、Cmax(7780 ng/mL) 和小鼠中的高暴露量 (AUCinf=3329 hng/mL)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12F36V cells[1]
Dosage: 35 mg/kg
Administration: Intraperitoneal injection (i.p.); once daily for 3 days
Result: Significantly reduced the bioluminescent signal 4 h after the first administration. The signal continuously decreased 4 h after each of the three administrations, and degradation was still evident 28 h after the final administration.
分子量

1247.54

Formula

C68H90N6O14S

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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dTAGV-1
目录号:
HY-145514D
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