PROTAC Axl Degrader 2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC Axl Degrader 2 

PROTAC Axl Degrader 2 是一种有效的选择性 PROTAC Axl 降解剂，IC50 为 1.61 µM。PROTAC Axl Degrader 2 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 2 诱导巨泡式细胞死亡 (mehuosis)。

PROTAC Axl Degrader 2

PROTAC Axl Degrader 2 Chemical Structure

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生物活性

PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis[1].

IC50 & Target

IC50: 1.61 µM (AXL)[1]
体外研究
(In Vitro)

PROTAC Axl Degrader 2 (compound 20) (72 h) shows anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 2 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 2 (1, 2 µM) reduces the expression of AXL, can be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 2 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 2 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 cells[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: MDA-MB-231, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.

体内研究
(In Vivo)

PROTAC Axl Degrader 2 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 2 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 7.80%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 2 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
20 i.v. 2 7581.3 279 0.82 1.18 0.72 –
p.o. 20 3592.1 144 2.25 4.43 – 7.80

6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.

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

Animal Model: Female balb/c nude mice (MDA-MB-231 xenografts)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection
Result: Did not induce systemic toxicity.
Animal Model: 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1]
Dosage:
Administration: 20 mg/kg for o.p.; 2 mg/kg for i.v.
Result: Showed an oral bioavailability of 7.80%.

分子量

713.79

Formula

C38H39N11O4
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]. Shi W, et al. Structure-based discovery of receptor tyrosine kinase AXL degraders with excellent anti-tumor activity by selectively degrading AXL and inducing methuosis. Eur J Med Chem. 2022; 234:114253.

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