2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. PROTAC EML4-ALK Degrader-2

PROTAC EML4-ALK Degrader-2 是一种 EML4-ALK PROTAC 降解。PROTAC EML4-ALK Degrader-2 对 ALK 表现出强效的选择性抑制活性，其 IC50 为 1.6 nM。PROTAC EML4-ALK 对 IGF1R、INSR、FLT3 和 FGFR2 表现出选择性。 PROTAC EML4-ALK Degrader-2 在体外和体内均具有抗癌活性。PROTAC EML4-ALK Degrader-2 可用于非小细胞肺癌 (NSLC)，肺癌和宫颈癌的研究。
(粉色: EML4-ALK 配体 (HY-15656)；蓝色: Cereblon 配体 (HY-10984)；黑色: 连接子 (HY-42776))。

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PROTAC EML4-ALK Degrader-2

PROTAC EML4-ALK Degrader-2 Chemical Structure

CAS No. : 2417174-28-6

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PROTAC EML4-ALK Degrader-2 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research[1][2]. (Pink: EML4-ALK ligand (HY-15656); Blue: Cereblon ligand (HY-10984); Black: linker (HY-42776)).

IC50 & Target[1]

EML4-ALK

 

体外研究
(In Vitro)

PROTAC EML4-ALK Degrader-2 (compound B3) (72 小时) 在正常人肝细胞系 LO2 中不增加对正常细胞的毒性，并在 H3122、H2228、H1299、A549 和 HeLa 细胞中显示出抗增殖作用，其 IC50 值分别为 0.3、0.9、2.84、1.6 和 1.18 μM[1]。
PROTAC EML4-ALK Degrader-2 (0-50 nM, 0-32 小时) 在 H3122 细胞中，能以浓度和时间依赖性方式降低 ALK 融合蛋白的细胞水平[1]。
PROTAC EML4-ALK Degrader-2 (10-500 nM) 对 ALK 显示出高选择性，对 IGF1R 和 INSR 保持中等抑制活性，但不诱导 IGF1R 和 INSR 的降解[1]。
PROTAC EML4-ALK Degrader-2 并非对 ALK 耐药突变有效：在 BaF3-ALK-L1196M 和 BaF3-ALK-G1202R 细胞中，它对 BaF3-ALK-L1196M 细胞的活性略优于LDK378 [1]。

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

PROTAC EML4-ALK Degrader-2 相关抗体:

Western Blot Analysis[1]

Cell Line: H3122 cells
Concentration: 0, 1, 5, 10, 20, 50 and 100 nM
Incubation Time: 0, 4, 8, 16, 24 and 32 h
Result: Degraded ALK in a dose dependent manner for 8 h; effectively degraded ALK at 50 nM for 8 h; degraded all the ALK protein at 200 nM.
Achieved amount (>80%) of EML4-ALK degradation after 16 h treatment at 100 nM.
Not observed maximum degradation of EML4-ALK degradation until 24 h at 100 nM.
Inhibited p-ALK and downregulated the level of p-STAT3 after 24 h at 100 nM.
Induced ALK degradation in a concentration dependent manner after 24 h.
Achieved maximum degradation of EML4-ALK degradation at 50 nM.
Downregulated the level of p-ALK and p-STAT3 in a concentration dependent manner after 24 h.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 1 mg/kg i.v. AUCall 1322 ng·h/mL
Rat[1] 1 mg/kg i.v. AUCinf 1409 ng·h/mL
Rat[1] 1 mg/kg i.v. T1/2 4.09 h
Rat[1] 1 mg/kg i.v. CL 16.3 mL/min/kg
Rat[1] 1 mg/kg i.v. Vss 1335 mL/kg
体内研究
(In Vivo)

PROTAC EML4-ALK Degrader-2 (compound B3) (25-50 mg/kg，口服，每日一次，持续 15 天) 在 H3122 异种移植瘤小鼠模型中，能以剂量依赖性方式抑制肿瘤生长，且安全性良好[1]。

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

Animal Model: H3122 cells (5 x 106) induced-female BALB/c nude mice (6-7 weeks) (18-22g) [1]
Dosage: 25, 50 mg/kg
Administration: o.p., once daily for 15 days
Result: Observed tumor growth inhibitions (TGIs) of 37% and 48% at dose of 25 mg/kg and 50 mg/kg, respectively.
Did not cause significant weight loss and toxicity.
分子量

1060.65

Formula

C52H66ClN9O11S
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

PROTAC EML4-ALK Degrader-2 相关分类

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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.

Keywords:

PROTAC EML4-ALK Degrader-22417174-28-6PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246H3122 cellselectiveanti-proliferation effectnon-small cell lung cancercervical cancerInhibitorinhibitorinhibit

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