GlpBio

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.

RET 相关产品(29)

  • GC10035 structure
    GC10035TG101209
    CAS: 936091-14-4
    纯度: >99.50%

    An inhibitor of JAK2, FLT3, RET, and JAK3

  • GC10111 structure
    GC10111Regorafenib
    CAS: 755037-03-7
    纯度: >99.00%

    Regorafenib是一种具口服活性的多激酶抑制剂，抑制VEGFR1/2/3，PDGFRβ，Kit，RET和Raf-1的IC 50 值分别为13/4.2/46，22，7，1.5和2.5nM。

  • GC10914 structure
    GC10914AST 487
    CAS: 630124-46-8
    纯度: >99.00%

    A multi-kinase inhibitor

  • GC14292 structure
    GC14292Apatinib Mesylate
    CAS: 811803-05-1
    纯度: >98.00%

    A selective VEGFR2 inhibitor

  • GC14534 structure
    GC14534Regorafenib monohydrate
    CAS: 1019206-88-2
    纯度: >99.50%

    A multi-kinase inhibitor

  • GC14606 structure
    GC14606Regorafenib hydrochloride
    CAS: 835621-07-3
    纯度: >99.50%

    A multi-kinase inhibitor

  • GC15454 structure
    GC15454Lenvatinib (E7080)
    CAS: 417716-92-8
    纯度: >99.50%

    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。

  • GC16391 structure
    GC16391Amuvatinib (MP-470, HPK 56)
    CAS: 850879-09-3
    纯度: >98.00%

    A multi-targeted RTK inhibitor

  • GC18492 structure
    GC18492GSK3179106
    CAS: 1627856-64-7
    纯度: >99.00%

    A RET kinase inhibitor

  • GC19062 structure
    GC19062BBT594
    CAS: 882405-89-2
    纯度: >99.50%

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

  • GC31780 structure
    GC31780Pralsetinib (Blu667)
    CAS: 2097132-94-8
    纯度: >98.50%

    Pralsetinib (Blu667)是转染重排（RET）激酶抑制剂，用于治疗特定的RET基因变异阳性肿瘤。

  • GC32797 structure
    GC32797AD80
    CAS: 1384071-99-1
    纯度: >99.50%

    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.

  • GC33362 structure
    GC33362Amuvatinib hydrochloride (MP470 hydrochloride)
    CAS: 1055986-67-8

    A multi-targeted RTK inhibitor

  • GC34159 structure
    GC34159Ilorasertib (ABT-348)
    CAS: 1227939-82-3

    A multi-kinase inhibitor

  • GC34509 structure
    GC34509BT-13
    CAS: 924537-98-4
    纯度: >99.50%

    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。

  • GC34809 structure
    GC34809SPP-86
    CAS: 1357349-91-7
    纯度: >99.50%

    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.

  • GC36438 structure
    GC36438Lenvatinib mesylate
    CAS: 857890-39-2
    纯度: >98.00% / >99.00%

    An inhibitor of VEGFR2 and VEGFR3

  • GC37047 structure
    GC37047Pz-1
    CAS: 1800505-64-9
    纯度: >99.00%

    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。

  • GC37933 structure
    GC37933WHI-P180 hydrochloride
    CAS: 153437-55-9

    A multi-kinase inhibitor

  • GC38519 structure
    GC38519Ilorasertib hydrochloride
    CAS: 1847485-91-9
    纯度: >98.50%

    A multi-kinase inhibitor

  • GC49686 structure
    GC49686N-desmethyl Regorafenib N-oxide
    CAS: 835621-12-0
    纯度: >90.00%

    An active metabolite of regorafenib

  • GC60592 structure
    GC60592APS6-45
    CAS: 2188236-41-9
    纯度: >99.50%

    APS6-45(Compound 10) is an orally active tumor-calibrated inhibitor (TCI) that inhibits RAS/MAPK signaling and exhibits antitumor activity.

  • GC64340 structure
    GC64340Zeteletinib
    CAS: 2216753-97-6

    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。

  • GC65354 structure
    GC65354Enbezotinib
    CAS: 2359649-81-1
    纯度: >99.00%

    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。