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Home >> Signaling Pathways >> Tyrosine Kinase

Tyrosine Kinase(酪氨酸激酶)

  1. Cat.No. 产品名称 Information
  2. GC33840 SU1498 (AG 1498)

    AG 1498; Tyrphostin SU 1498

     A selective inhibitor of VEGFR2/FLK1
  3. GC33519 2,5-Dihydroxybenzoic acid

    2,5-二羟基苯甲酸

     A benzoic acid with diverse biological activities
  4. GC33368 BCR-ABL-IN-2 BCR-ABL-IN-2是BCR-ABL1激酶的抑制剂，其对ABL1native和ABL1T315I的IC50值分别为57nM，773nM。
  5. GC33362 Amuvatinib hydrochloride (MP470 hydrochloride)

    MP470 hydrochloride; HPK 56 hydrochloride

     A multi-targeted RTK inhibitor
  6. GC33361 DDR Inhibitor DDRInhibitor是一种高效的盘状结构域受体(discoidindomainreceptor)抑制剂，对DDR2的IC50值为3.3nM，在浓度为1.5nM时，对DDR1有53%的抑制作用。
  7. GC33352 CP-547632

    3-[(4-溴-2,6-二氟苄基)氧基]-5-[3-[4-(吡咯烷-1-基)丁基]脲基]异噻唑-4-甲酰胺

     A potent inhibitor of VEGFR2 and bFGF
  8. GC33351 CZC-8004 (CZC-00008004)

    N2-(4-(氨甲基)苯)-5-氟-N4-苯基嘧啶-2,4-二胺,CZC-00008004

     A tyrosine kinase inhibitor
  9. GC33343 BCR-ABL-IN-1 BCR-ABL-IN-1是一种BCR-ABL酪氨酸激酶抑制剂，pIC50值为6.46，可能用于慢性髓细胞白血病的研究。
  10. GC33319 2-Keto Crizotinib (PF-06260182)

    克里唑替尼杂质,PF-06260182

     2-Keto Crizotinib (PF-06260182) (PF-06260182) 是 crizotinib 的活性内酰胺代谢物。
  11. GC33297 DDR1-IN-3 DDR1-IN-3 是一种选择性 Discoidin Domain Receptor 1 (DDR1) 抑制剂，IC50 值为 9.4 nM。 DDR1-IN-3 也抑制 TRK 家族。
  12. GC33273 TAS-115 mesylate (TAS-115 methanesulfonate)

    TAS-115 mesylate

     A multi-kinase inhibitor
  13. 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。
  14. GC33266 JNJ-38877618 JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50).
  15. GC33246 AZD3229 Tosylate An inhibitor of c-Kit-driven cell proliferation
  16. GC33242 FLT3-IN-1 Succinate FLT3-IN-1Succinate是有效地FLT3抑制剂，来自专利WO2015056683A1，化合物实例A。
  17. GC33241 CSF1R-IN-1 CSF1R-IN-1 is a CSF1R (Colony Stimulating Factor 1 Receptor) inhibitor with an IC50 of 0.5 nM in vitro kinase activity assay.
  18. GC33203 c-Met-IN-2 c-Met-IN-2是一种有效的，选择性的，可口服的c-Met抑制剂，IC50值为0.6nM，具有抗肿瘤活性。
  19. GC33201 GZD856 GZD856是一种新型，有口服活性的PDGFRα/β抑制剂，IC50分别为68.6和136.6nM。具有抗肺癌活性。也是Bcr-AblT315I的抑制剂，对Bcr-Abl和T315I突变型的IC50分别为19.9和15.4 nM。
  20. GC33195 EGFR-IN-2 EGFR-IN-2是一种非共价的，不可逆的，突变选择性的二代EGFR抑制剂。
  21. GC33190 Ensartinib (X-396)

    X-396

     An ALK inhibitor
  22. GC33189 SAR125844 SAR125844 is a potent intravenously active and highly selective Met (c-Met) kinase inhibitor, displaying nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and H1094Y, Y1235D, M1250T, L1195V, and D1228H kinase domain mutants (IC50 values of 0.22, 1.7, 6.5, 65, and 81 nmol/L, respectively).
  23. GC33181 T338C Src-IN-2

    T338CSrc-IN-2是突变型c-Src激酶抑制剂，IC50值317nM，还能抑制T338C/V323A和T338C/V323S双突变Src活性，IC50值57和19nM。
  24. GC33173 TAS-115

    TAS-115

     A multi-kinase inhibitor
  25. GC33172 BGB-102 (JNJ-26483327)

    17-溴-1,8,9,10,11,12,13,14-八氢-20-甲氧基-13-甲基-4,6-乙烯桥嘧啶并[4,5-B][6,1,12]苯并氧杂二氮杂环十五碳七烯,JNJ-26483327

     BGB-102 (JNJ-26483327) 是一种有效的多激酶抑制剂，针对 EGFR、HER2 和 HER4，IC50 分别为 9.6 nM、18 nM 和 40.3 nM。
  26. GC33171 ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
  27. GC33168 T338C Src-IN-1 T338CSrc-IN-1是突变型c-SrcT338C高效抑制剂，IC50值111nM。对WTSrc活性弱10倍以上。
  28. GC33141 SKLB4771 (FLT3-IN-1)

    FLT3-?IN-?1

     SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10?nM.
  29. GC33131 NRC-2694 NRC-2694是一种表皮生长因子受体(EGFR)拮抗剂，具有抗癌、抗增殖的活性。
  30. GC33112 CH7057288 CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.
  31. GC33096 AST2818 mesylate

    甲磺酸伏美替尼; Furmonertinib mesylate; AST2818 mesylate

     An inhibitor of mutant EGFRs
  32. GC33090 AZ-23 (AZ23)

    5-氯-N-[(1S)-1-(5-氟吡啶-2-基)乙基]-N'-(5-异丙氧基-1H-吡唑-3-基)嘧啶-2,4-二胺,AZ23; AZ 23

     AZ-23 (AZ23) 是一种 ATP 竞争性和口服生物可利用的 Trk 激酶 A/B/C 抑制剂，IC50 为 2 nM (TrkA)、8 nM (TrkB)、24 nM (FGFR1)、52 nM (Flt3)、55分别为 nM (Ret)、84 nM (MuSk)、99 nM (Lck)。
  33. GC33087 2,4-Pyrimidinediamine with linker

    N2-[4-[(3-氨基丙基)氨基]苯基]-N4-(5-环丙基-1H-吡唑-3-基)-2,4-嘧啶二胺

     A multi-kinase inhibitor
  34. GC33086 LDN-192960

    3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺

     An inhibitor of haspin and DYRK2
  35. GC33072 AZ7550 An active metabolite of AZ 9291
  36. GC33064 CG-806 (Luxeptinib)

    CG-806

     CG-806 (Luxeptinib) (CG-806) 是一种具有口服活性、可逆、一流、非共价且有效的 pan-FLT3/pan-BTK 抑制剂。 CG-806 (Luxeptinib) 在急性髓性白血病细胞中诱导细胞周期停滞、凋亡或自噬。
  37. GC33062 JH-VIII-157-02 JH-VIII-157-02是alectinib的结构类似物，为ALK抑制剂，对棘皮动物微管相关蛋白样4(EML4)-ALKG1202R的IC50值为2nM。
  38. GC33061 Rociletinib hydrobromide (CO-1686 (hydrobromide))

    CO-1686氢溴酸盐,CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide

     Rociletinib hydrobromide (CO-1686 (hydrobromide)) (CO-1686 hydrobromide) 是一种口服激酶抑制剂，特异性靶向 EGFR 的突变形式，包括 T790M，EGFRL858R/T790M 和 EGFRWT 的 Ki 值为 21.5 nM 和 303.3 nM，分别。
  39. GC33054 AZ1495 AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively.
  40. GC33053 HS-10296 hydrochloride

    盐酸阿美替尼; HS-10296 hydrochloride

     Almonertinib (HS-10296) hydrochloride 是一种口服的、不可逆的第三代 EGFR 酪氨酸激酶抑制剂，对 EGFR 致敏和 T790M 耐药突变具有高选择性。 HS-10296 hydrochloride 对 T790M、T790M/L858R 和 T790M/Del19 具有很强的抑制活性（IC50 分别为 0.37、0.29 和 0.21 nM），而对野生型的抑制效果较差（3.39 nM）。 HS-10296 hydrochloride 用于非小细胞肺癌的研究。
  41. GC33049 FN-1501 FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (CDK), with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively.
  42. GC33048 Epertinib (S-22611)

    艾培替尼,S-22611

     Epertinib (S-22611) (S-22611) 是一种有效的、口服的、可逆的、选择性的 EGFR、HER2 和 HER4 酪氨酸激酶抑制剂，IC50 分别为 1.48 nM、7.15 nM 和 2.49 nM。 Epertinib (S-22611) 显示出有效的抗肿瘤活性。
  43. GC33045 NAMI-A NAMI-A是一种钌基试剂，其特征在于对肿瘤转移的选择性活性，抑制粘附和迁移。
  44. GC33041 Gusacitinib (ASN-002)

    ASN-002

     A dual inhibitor of JAKs and Syk family kinases
  45. GC33027 AZD3229 An inhibitor of c-Kit-driven cell proliferation
  46. GC33022 Naquotinib (ASP8273)

    ASP8273

     An irreversible inhibitor of mutant EGFRs
  47. GC33020 CHMFL-BMX-078 (CHMFL-BMX 078)

    CHMFL-BMX 078

     An irreversible BMX inhibitor
  48. GC33004 Cediranib maleate (AZD-2171 maleate)

    西地尼布马来酸盐; AZD-2171 maleate

     An inhibitor of VEGF receptor tyrosine kinases
  49. GC32995 JNJ-47117096 hydrochloride (MELK-T1 hydrochloride)

    MELK-T1 hydrochloride

     JNJ-47117096 hydrochloride (MELK-T1 hydrochloride) 是有效的选择性 MELK 抑制剂，IC50 为 23 nM，也有效抑制 Flt3，IC50 为 18 nM。
  50. GC32992 7-Hydroxy-4-chromone (7-Hydroxychromone)

    7-羟基色原酮,7-Hydroxychromone

     7-Hydroxychromone is an inhibitor of Src kinase with IC50 of <300 μM.
  51. GC32989 Pyrotinib dimaleate (SHR-1258 dimaleate)

    马来酸吡咯替尼,SHR-1258 dimaleate

     Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.

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