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TAM Receptor(TAM受体)

TAM receptors (Tyro3, Axl, and Mer) belong to a family of receptor tyrosine kinases that have important effects on hemostasis and inflammation. TAM receptors affect cell proliferation, survival, adhesion, and migration. TAM receptors can be activated by the vitamin K-dependent proteins Gas6 and protein S. Protein S is more commonly known as an important cofactor for protein C as well as a direct inhibitor of multiple coagulation factors.

The TAM receptors-Tyro3, Axl, and Mer-comprise a unique family of receptor tyrosine kinases, in that as a group they play no essential role in embryonic development. TAM receptor signaling plays an especially important role in the engulfment and phagocytic clearance of apoptotic cells (ACs) and membranes in adult tissues.

Products for  TAM Receptor

  1. Cat.No. 产品名称 Information
  2. GC69061 Enapotamab Enapotamab 是一种 AXL/UFO 相关抗体,可用于合成 Bcl-xl 抑制剂抗体活性分子偶联物。
  3. GC68342 Tilvestamab Tilvestamab (BGB149) 是一种人源化抗 AXL 抗体,阻断 AXL 介导的细胞信号传导。Tilvestamab 在体外能显著抑制 Gas6 刺激诱导的 AXL 激活,并抑制 786-0-Luc RCC 细胞中下游 AXL 的磷酸化。Tilvestamab可用于癌症,尤其是 AXL 过度表达肾细胞癌的研究。
  4. GC67878 TL4830031 TL4830031 (compound 8i) 是一种喹诺酮类抗生素衍生物,是一种有效的 Axl 抑制剂,其 IC50 值为 26 nM。TL4830031 抑制 Axl 的磷酸化。TL4830031 抑制细胞侵袭和迁移。TL4830031 可用于癌症研究。
  5. GC64385 RU-302 RU-302 是一种非选择性的TAM 抑制剂,阻断 TAM Ig1 胞外域和 Gas6 Lg 结构域之间的界面。RU-302 用低微摩尔 IC50 有效阻断 Gas6 诱导的 Axl 受体活化,并有效抑制肺癌肿瘤的生长。
  6. GC64071 AZ14145845 AZ14145845 是一种具有体内药效的高选择性I1/2型Mer/Axl双特异性激酶抑制剂。
  7. GC62597 DS-1205b free base DS-1205b free base 是一种有效和选择性的 AXL 激酶抑制剂,IC50 值为 1.3 nM。DS-1205b free base 还可以抑制 MER,MET 和 TRKA,IC50 值分别为 63、104 和 407 nM。 DS-1205b free base 可以抑制细胞迁移和肿瘤生长。
  8. GC62516 UNC5293 UNC5293 是一种 MERTK 选择性的有效抑制剂 (Ki=190 pM)。UNC5293 抑制 MERTK (IC50=0.9 nM),对 Axl、Tyro3 和 Flt3 更具选择性。UNC5293 表现出优异的小鼠药代动力学特性,并可以被用于骨髓白血病研究。
  9. GC62266 XL092 XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
  10. GC38580 RU-301 RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively.
  11. GC37858 UNC2541 UNC2541 is a potent and specific inhibitor of Mer tyrosine kinase (MerTK) that binds in the MerTK ATP pocket with IC50 of 4.4 nM. UNC2541 inhibits phosphorylated MerTK (pMerTK) with EC50 of 510 nM.
  12. GC37733 TAM-IN-2 TAM-IN-2 是专利 US 20170275290 A1 中提到的 TAM 抑制剂,吡咯并三嗪化合物 0904。
  13. GC36744 Ningetinib Tosylate A multi-kinase inhibitor
  14. GC36135 Gilteritinib hemifumarate A FLT3 inhibitor
  15. GC33271 R916562 R916562是有效的和有选择性的Axl/VEGF-R2双重抑制剂,IC50值分别为136和24nM。
  16. GC19482 Gilteritinib A FLT3 inhibitor
  17. GC19330 SGI-7079 An Axl kinase inhibitor
  18. GC19166 Glesatinib hydrochloride Glesatinib hydrochloride (MGCD265 hydrochloride) 是一种具有口服活性的强效 MET/SMO 双重抑制剂。 Glesatinib hydrochloride 是一种酪氨酸激酶抑制剂,可拮抗 P-糖蛋白 (P-gp) 介导的非小细胞肺癌 (NSCLC) 中的多药耐药 (MDR)。
  19. GC19102 CEP-40783 A multi-kinase inhibitor
  20. GC18211 Ningetinib A multi-kinase inhibitor
  21. GC10408 2-D08 An inhibitor of sumoylation
  22. GC14488 NPS-1034 A dual MET/AXL inhibitor
  23. GC14218 TP-0903 An Axl kinase inhibitor
  24. GC14241 LDC1267 A TAM family kinase inhibitor
  25. GC13500 UNC2881 A Mer kinase inhibitor
  26. GC17793 UNC2250 A selective Mer kinase inhibitor
  27. GC17618 R428

    R428, as a Axl inhibitor, blocks Axl autophosphorylation on its C-terminal docking site, Tyr821, at nanomolar concentrations[1].

  28. GC14214 BMS-777607 A Met kinase family inhibitor
  29. GC15779 Cabozantinib (XL184, BMS-907351) A VEGFR2 inhibitor

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