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Home >> Signaling Pathways >> Tyrosine Kinase >> RET

RET

RET (REarranged during Transfection) is a receptor protein tyrosine kinase, which activates multiple signal transduction pathways. RET protein is composed of three domains: an extracellular ligand-binding domain, a transmembrane domain, and a cytoplasmic tyrosine kinase domain. The RET receptor tyrosine kinase (RTK) regulates key aspects of cellular proliferation and survival by regulating the activity of the mitogen- activated protein kinase (MAPK) and PI3K/Akt signaling pathways. RET also interacts directly with other kinases such as the epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (MET) and the focal adhesion kinase (FAK). Furthermore, BRAF and p38MAPK are downstream targets of RET. Kinase inhibitors that simultaneously inhibit RET and its downstream targets.

RET tyrosine kinase receptor presents an attractive therapeutic target for the treatment of certain cancer subsets. Deregulated RET activity has been identified as a causative factor in the development, progression and response to therapy of thyroid carcinoma. Elevated RET expression has been associated with the development of endocrine resistance in human breast cancer.

Products for  RET

  1. Cat.No. 产品名称 Information
  2. GC73196 RET-IN-21 RET-IN-21是受体酪氨酸激酶（RET）抑制剂，IC50为4.4 μM，具有抗肿瘤活性。
  3. GC68812 BT44 BT44 是选择性 RET 活化剂。BT44 可穿透血脑屏障，可用于研究神经退行性疾病及糖尿病。
  4. GC68623 AD57 AD57 是一种具有口服活性的多种激酶抑制剂，抑制 RET、BRAF、S6K 和 Src 活性，但对 mTOR 的活性明显减弱。
  5. GC68396 Vepafestinib Vepafestinib (compound 6) 是 RET 的抑制剂 (信息来自专利 WO2019039439)。
  6. GC67917 RET-IN-7 RET-IN-7 在体外显示出强大的 RET 激酶抑制作用，在体内对 RET 驱动的肿瘤异种移植物具有强大的疗效。
  7. GC65354 Enbezotinib Enbezotinib 是一种 RET 的抑制剂，可抑制 RET 的自磷酸化。Enbezotinib 可用于癌症的研究。
  8. GC64340 Zeteletinib

    BOS-172738; DS-5010

     Zeteletinib (BOS-172738; DS-5010) 是一种口服有效的，选择性 RET 激酶抑制剂，对 RET 具有纳摩尔效力，对 VEGFR2 具有 >300 倍的选择性。Zeteletinib 对野生型 RET、RETV804M/L gatekeeper 突变体和最常见的致癌 RET 突变体 M918T 显示出较高的效力。Zeteletinib 具有强大的抗肿瘤活性。
  9. GC49686 N-desmethyl Regorafenib N-oxide

    瑞戈非尼杂质14

     An active metabolite of regorafenib
  10. GC60592 APS6-45 APS6-45(Compound 10) is an orally active tumor-calibrated inhibitor (TCI) that inhibits RAS/MAPK signaling and exhibits antitumor activity.
  11. GC38519 Ilorasertib hydrochloride

    ABT-348 hydrochloride

     A multi-kinase inhibitor
  12. GC37933 WHI-P180 hydrochloride

    Janex 3 hydrochloride;

     A multi-kinase inhibitor
  13. GC37047 Pz-1 Pz-1是有效地 RET 和 VEGFR2 受体酪氨酸激酶抑制剂，Pz-1抑制这两个野生型激酶的 IC50 值小于 1 nM。
  14. GC36438 Lenvatinib mesylate

    仑伐替尼甲酸盐; E7080 mesylate

     An inhibitor of VEGFR2 and VEGFR3
  15. GC34809 SPP-86 SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
  16. GC34509 BT-13 BT-13是有效的、胶质细胞源性神经营养因子(GDNF)受体RET的选择性激动剂(独立于GDNF配体发挥作用)，促进体外感觉神经元神经突生长，减轻大鼠神经病变的发生。
  17. GC34159 Ilorasertib (ABT-348)

    ABT-348

     A multi-kinase inhibitor
  18. GC33362 Amuvatinib hydrochloride (MP470 hydrochloride)

    MP470 hydrochloride; HPK 56 hydrochloride

     A multi-targeted RTK inhibitor
  19. GC32797 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
  20. GC31780 Pralsetinib (Blu667)

    普拉替尼; BLU-667

    Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).
  21. GC19062 BBT594

    NVP-BBT594

     BBT594 是一种有效的受体酪氨酸激酶 RET 抑制剂，用于癌症治疗。
  22. GC18492 GSK3179106

    RET Kinase Inhibitor 1

     A RET kinase inhibitor
  23. GC14292 Apatinib Mesylate

    阿帕替尼

    A selective VEGFR2 inhibitor
  24. GC15454 Lenvatinib (E7080)

    仑伐替尼; E7080

     E7080，称为乐伐替尼，是一种口服多靶点酪氨酸激酶抑制剂，包括 VEGF、FGF 和 SCF 受体，已被证明可以提高放射性碘难治性甲状腺癌患者的生存率。
  25. GC10111 Regorafenib

    瑞戈非尼; BAY 73-4506

     A multi-kinase inhibitor
  26. GC14534 Regorafenib monohydrate

    瑞格非尼一水合物,BAY 73-4506 monohydrate

     A multi-kinase inhibitor
  27. GC14606 Regorafenib hydrochloride

    瑞戈非尼盐酸盐; BAY 73-4506 hydrochloride

     A multi-kinase inhibitor
  28. GC10914 AST 487

    NVP-AST 487

     A multi-kinase inhibitor
  29. GC16391 Amuvatinib (MP-470, HPK 56)

    N-(1,3-苯并二氧戊环-5-基甲基)-4-苯并呋喃并[3,2-D]嘧啶-4-基-1-哌嗪硫代甲酰胺,MP470,MP 470,HPK56

     A multi-targeted RTK inhibitor
  30. GC10035 TG101209

    N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺,TG-101209

     An inhibitor of JAK2, FLT3, RET, and JAK3

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