EGFR/HER2

Inhibitory Selectivity
Catalog No.Inhibitor Name EGFR/ErbB1HER2/ErbB2ErbB3ErbB4Other
A10362Erlotinib HCl
****
A10422Gefitinib
**
A10514Lapatinib Ditosylate
**
**
*
c-Src
A10141Afatinib
****
**
A10638Neratinib
*
*
KDR,Src
A10211Canertinib
****
***
A11752Lapatinib
**
**
*
c-Src
A10047AG-490
*
*
JAK2
A10242CP-724714
**
A11051Dacomitinib
***
*
*
A10991WZ4002
****
***
A10116Sapitinib
***
***
HDAC,HDAC1,HDAC6
A10246CUDC-101
***
**
A11022AG-1478
***
A10702PD153035 HCl
****
Src,MEK/ERK,Raf
A10706Pelitinib
*
*
c-Abl,FLT1,c-Fms
A10043AEE788
****
***
*
MEK,LCK,VEGFR2
A11209AC480
**
*
*
A10678OSI-420
****
A10990WZ3146
****
A11155AST-1306
****
***
****
A13028Rociletinib
**
A11158Varlitinib
***
****
A13825Icotinib
***
MEK1,Aurora B,LCK
A11236TAK-285
**
**
*
Src,VEGFR,JAK3
A14049WHI-P154
***
A12725PD168393
****
A13755CNX-2006
**
PDGFR
A11949Tyrphostin 9
*
A15940AG-18
*
A15551AZD3759
****
A14985Afatinib Dimaleate
****
**
A13146CL-387785
****
A13044Poziotinib
***
***
**
A13681Osimertinib
**
BLK,ACK1,BRK
A15516AZ5104
****
***
A10992WZ8040
topo II
A10426Genistein
A12448Butein
mTOR
A10210Chrysophanic Acid
A10053Tyrphostin AG 879
*
Trk
A10286Daphnetin
*
PKC, PKA
A11027Irbinitinib (ARRY-380, ONT-380)
****
A11028AV-412
***
*
A11334BIBX 1382
****
*
A12867CGP-52411
*
A13588Tyrphostin AG 183
*
A15509WHI-P180
*
Cdk2
A10612Mubritinib (TAK 165)
****
A16413ARRY-380 (Irbinitinib)
****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

产品 51 到 100 共 105个

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  1. Poziotinib

    Catalog No. A13044
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    EGFR 抑制剂
    Poziotinib是一种口服生物利用的,基于喹唑啉的泛表皮生长因子受体(EGFR或HER)抑制剂,具有潜在的抗肿瘤活性。 了解更多
  2. EGFR Inhibitor

    Catalog No. A13673
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    EGFR 抑制剂
    EGFR inhibitor是一种可透过细胞的4,6-二取代嘧啶化合物,可选择性抑制EGFR激酶,在体外的IC50值为21 nM,可阻断细胞中的受体自身磷酸化。 了解更多
  3. Epidermal Growth Factor Receptor Peptide (985-996)

    Catalog No. A14877
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    Epidermal Growth Factor Receptor Peptide (985-996)存在于细胞表面,并通过其特定配体(包括表皮生长因子和转化生长因子)的结合而被激活。 了解更多
  4. Compound 56

    Catalog No. A14953
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    EGFR 抑制剂
    Compound 56是EGFR酪氨酸激酶活性的细胞渗透性,可逆性和ATP竞争性抑制剂。 了解更多
  5. Afatinib dimaleate

    Catalog No. A14985
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    EGFR 抑制剂
    Afatinib dimaleate是一种不可逆的EGFR/HER2抑制剂,对于HER2的体外药效IC50为14 nM。 了解更多
  6. Erlotinib mesylate

    Catalog No. A15081
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    EGFR 抑制剂
    Erlotinib mesylate是人EGFR酪氨酸激酶的直接作用抑制剂,IC50为2 nM。 了解更多
  7. Gefitinib hydrochloride

    Catalog No. A15093
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    EGFR 抑制剂
    Gefitinib hydrochloride是一种EGFR抑制剂,可通过靶细胞中的表皮生长因子受体(EGFR)中断信号传导。因此,它仅在EGFR突变和过度活跃的癌症中有效。 了解更多
  8. Vandetanib trifluoroacetate

    Catalog No. A15272
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    VEGFR/EGFR 抑制剂
    Vandetanib trifluoroacetate是一种有效的VEGFR2抑制剂,IC50为40 nM。 了解更多
  9. WHI-P180

    Catalog No. A15509
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    EGFR/Cdk2 抑制剂
    WHI-P180是有效的EGFR和Cdk2抑制剂,IC50分别为4.0和1.0 uM。 了解更多
  10. AZ5104

    Catalog No. A15516
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    EGFR 抑制剂
    AZD-9291的去甲基代谢产物AZ5104是一种有效的EGFR抑制剂,对于EGFR(L858R/T790M),EGFR(L858R),EGFR(L861Q)和EGFR,IC50 <1 nM,6 nM,1 nM和25 nM EGFR(野生型)。 了解更多
  11. D-69491

    Catalog No. A15457
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    HER2 抑制剂
    D-69491 (SU11464)是一种小分子HER2抑制剂,正在开发中,用于治疗HER2高表达的肿瘤,例如乳腺癌,卵巢癌,肺癌和胰腺癌。 了解更多
  12. AZD3759

    Catalog No. A15551
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    EGFR 抑制剂
    AZD3759是表皮生长因子受体(EGFR)的口服抑制剂。它结合并抑制EGFR以及某些突变形式的EGFR的活性。 了解更多
  13. ASP8273 (Naquotinib)

    Catalog No. A14408
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    irreversible EGFR 抑制剂
    ASP8273 (Naquotinib)是不可逆的,第三代,选择性突变的表皮生长因子受体(EGFR)抑制剂,具有潜在的抗肿瘤活性。 了解更多
  14. EGF816 (Nazartinib)

    Catalog No. A14416
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    EGFR T790M 抑制剂
    EGF816 (Nazartinib)是新型的突变选择性EGFR共价抑制剂。克服了NSCLC中T790M介导的耐药性。 了解更多
  15. CL-387785 (EKI-785)

    Catalog No. A13146
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    EGFR 抑制剂
    CL-387785是EGFR的不可逆抑制剂,IC50为370+/-120 pM;能够在功能水平上克服由T790M突变引起的抗药性。 了解更多
  16. AG-18 (Tyrphostin 23)

    Catalog No. A15940
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    EGFR 抑制剂
    AG-18 (Tyrphostin 23)是人表皮癌细胞系A431中的表皮生长因子(EGF)受体激酶抑制剂,IC50值为35M。 了解更多
  17. DM1-SMCC

    Catalog No. A15955
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    potent EGFR 抑制剂
    DM1-SMCC是具有反应性接头SMCC的DM1,后者可与抗体反应以形成抗体-药物偶联物。 了解更多
  18. PD168393

    Catalog No. A12725
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    EGFR 抑制剂
    PD168393是一种有效的,细胞可渗透的,不可逆的EGFR抑制剂,IC50值为700 pM。 了解更多
  19. EAI045

    Catalog No. A16193
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    EGFR inhbitor
    EAI045是一种有效的选择性EGFR抑制剂。EAI045靶向选定的耐药性EGFR突变体,但保留了野生型受体。 了解更多
  20. PD158780

    Catalog No. A16254
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    EGFR 抑制剂
    PD158780是一种非常有效的EGFR抑制剂,IC50为0.08 nM。泛特异性的ErbB受体拮抗剂。 了解更多
  21. TX1-85-1

    Catalog No. A16361
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    Her3 (ErbB3) ligand
    TX1-85-1是ErbB3抑制剂。TX2-121-1可能通过变构机制发挥Her3依赖的药理作用,从而破坏Her3与其他蛋白质(例如Her3或cMet)之间的相互作用,与此处介绍的结果一致,并且与阻断催化功能的常规激酶抑制剂不同。 了解更多
  22. ARRY-380 (Irbinitinib)

    Catalog No. A16413
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    HER2 抑制剂
    ARRY-380是人表皮生长因子受体酪氨酸激酶ErbB-2(也称为HER2)的口服生物利用抑制剂,具有潜在的抗肿瘤活性。 了解更多
  23. Erlotinib

    Catalog No. A11416
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    EGFR 抑制剂
    Erlotinib是一种表皮生长因子受体抑制剂(EGFR抑制剂),抑制纯化 EGFR 激酶的 IC50 为2 nM。厄洛替尼以可逆方式与受体的三磷酸腺苷(ATP)结合位点结合。为了传递信号,需要将两个EGFR分子聚在一起形成同型二聚体。然后,这些分子利用ATP分子在酪氨酸残基上彼此进行反磷酸化,从而产生磷酸酪氨酸残基,将磷酸酪氨酸结合蛋白募集到EGFR,从而组装将信号级联转导至细胞核或激活其他细胞生化过程的蛋白复合物。当厄洛替尼与EGFR结合时,就不可能在EGFR中形成磷酸酪氨酸残基,并且不会引发信号级联。 了解更多
  24. AG-1517

    Catalog No. A13001
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    EGFR 抑制剂
    AG 1517是表皮生长因子受体酪氨酸激酶EGFR的有效和选择性ATP竞争性抑制剂。 了解更多
  25. AV412

    Catalog No. A15460
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    EGFR 抑制剂
    AV-412 (MP412)是一种EGFR抑制剂,对EGFR,EGFRL858R,EGFRT790M,EGFRL858R/T790M和ErbB2的IC50分别为0.75、0.5、0.79、2.3、19 nM。 了解更多
  26. Avitinib (AC0010)

    Catalog No. A16826
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    irreversible EGFR 抑制剂
    Avitinib (AC0010)是一种基于吡咯并嘧啶的不可逆EGFR抑制剂,对EGFR L858R/T790M双重突变具有突变选择性,IC50值为0.18 nM,效力比野生型EGFR(IC50值为7.68 nM)高近43倍。它具有可比的抗肿瘤活性和耐受的毒性。 了解更多
  27. Lazertinib (YH25448,GNS-1480)

    Catalog No. A16827
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    EGFR 抑制剂
    Lazertinib (YH25448,GNS-1480)是一种有效的,高度突变选择性和不可逆的EGFR-TKI,对于Del19/T790M,L858R/T790M,Del19,Del19,IC50值分别为1.7 nM,2 nM,5 nM,20.6 nM和76 nM。L85R和野生型EGFR分别显示出更高的IC50值,即抗药性ErbB2和ErbB4。 了解更多
  28. Tyrphostin AG-528

    Catalog No. A17072
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    EGFR 抑制剂
    Tyrphostin AG-528,也称为Tyrphostin B66,是EGFR蛋白酪氨酸激酶抑制剂。 了解更多
  29. Pyrotinib Racemate

    Catalog No. A17068
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    EGFR/HER2 dual 抑制剂
    Pyrotinib Racemate是吡罗替尼的外消旋体。吡罗替尼是一种有效的选择性EGFR/HER2双重抑制剂。 了解更多
    • 最新产品

    AG-494

    Catalog No. A17142
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    EGFR 抑制剂
    AG-494是表皮生长因子受体激酶的抑制剂,在HT-22细胞中的IC50值为1μM。 了解更多
  30. Lavendustin A

    Catalog No. A17119
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    EGFR 抑制剂
    Lavendustin A是表皮生长因子(EGF)受体相关酪氨酸激酶的选择性抑制剂,IC50值为11 nM。 了解更多
  31. AG-99

    Catalog No. A17123
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    EGFR 抑制剂
    AG-99是一种表皮生长因子受体(EGFR)激酶抑制剂,IC50值为10μM。 了解更多
  32. AG 555

    Catalog No. A18337
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    EGFR 抑制剂
    AG555 is a potent epidermal growth factor receptor (EGFR) kinase inhibitor. 了解更多
  33. RG14620

    Catalog No. A18327
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    EGFR 抑制剂
    RG14620 is an EGFR inhibitor with an IC50 of 3 μM. 了解更多
  34. MTX-211

    Catalog No. A18324
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    EGFR/PI3K 双重抑制剂
    MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer. 了解更多
  35. DBPR112

    Catalog No. A18857
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    EGFR 抑制剂
    DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. 了解更多
  36. EGFR-IN-7

    Catalog No. A18562
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    EGFR 抑制剂
    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity. 了解更多
  37. Mutated EGFR-IN-2

    Catalog No. A18565
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    EGFR 抑制剂
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity. 了解更多
  38. Genistein

    Catalog No. A10425
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    EGFR inhibitor
    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis. 了解更多
  39. NSC 228155

    Catalog No. A16638
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    EGFR activator
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. 了解更多
  40. Epertinib

    Catalog No. A13777
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    EGFR/HER2/HER4 inhibitor
    Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity. 了解更多
  41. EGFR-IN-2

    Catalog No. A12628
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    EGFR inhibitor
    EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor. 了解更多
  42. CHMFL-EGFR-202

    Catalog No. A12524
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    EGFR inhibitor
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. 了解更多
  43. EGFR-IN-3

    Catalog No. A15847
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    EGFR inhibitor
    EGFR-IN-3 is an epidermal growth factor receptor (EGFR) inhibitor. 了解更多
  44. Canertinib dihydrochloride

    Catalog No. A11344
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    EGFR inhibitor
    Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. 了解更多
  45. Afatinib

    Catalog No. A18014
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    EGFR inhibitor
    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. 了解更多
  46. Tarloxotinib bromide

    Catalog No. A20849
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    EGFR/HER2 inhibitor
    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor. 了解更多
  47. Mutant EGFR inhibitor

    Catalog No. A21144
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    EGFR inhibitor
    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M. 了解更多
  48. HS-10296 hydrochloride

    Catalog No. A21661
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    EGFR/T790M inhibitor
    HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR. 了解更多
  49. AST2818 mesylate

    Catalog No. A21666
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    EGFR inhibitor
    AST2818 mesylate is an EGFR inhibitor. 了解更多

产品 51 到 100 共 105个

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