Bcr-Abl

Catalog No.Inhibitor Name Bcr-AblAblOther
A10290Dasatinib
****
****
Src,c-Kit (D816V),c-Kit (wt)
A10468Imatinib Mesylate
*
c-Kit,PDGFR
A10108Saracatinib
**
c-Src,LCK,EGFR (L861Q)
A10080Ponatinib
****
****
PDGFRα,VEGFR2,FGFR1
A10644Nilotinib
**
A10715Danusertib
**
**
Aurora A,TrkA,RET
A10095AT9283
***
JAK3,JAK2,Aurora B
A10988Degrasyn
*
DUB
A10119Bafetinib
***
***
Lyn
A10508KW-2449
**
***
FLT3 (D835Y),FLT3,FGFR1
A10661NVP-BHG712
*
EphB4,C-Raf,c-Src
A11200Rebastinib
***
FLT3,KDR,Tie-2
A15849GZD824 Dimesylate
****
****
A11439GNF-2
*
A15887GNF-7
***
*
A13029Radotinib
**
A16320Dasatinib Monohydrate
****
****
Src,c-Kit (D816V),c-Kit (wt)
A13237GNF-5
*
A13120PD173955
***
Src
A11379DPH
A13530Flumatinib mesylate
****
PDGFRβ, c-Kit

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.

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  1. BCR-ABL-IN-2

    Catalog No. A21043
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    inhibitor of BCR-ABL1 tyrosine kinase
    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively. 了解更多
  2. 1-Naphthyl PP1 hydrochloride

    Catalog No. A21790
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    Src/c-Abl inhibitor
    1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). 了解更多
  3. CHMFL-ABL/KIT-155

    Catalog No. A12421
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    ABL/c-KIT dual kinase inhibitor
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor. 了解更多
  4. BCR-ABL-IN-1

    Catalog No. A12496
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    BCR-ABL inhibitor
    BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia. 了解更多
  5. CHMFL-ABL-039

    Catalog No. A13182
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    BCR-ABL inhibitor
    CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia. 了解更多
  6. CHMFL-ABL-121

    Catalog No. A19079
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    ABL2 inhibitor
    CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively. 了解更多
  7. CZC-8004

    Catalog No. A19444
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    ABL inhibitor
    CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase. 了解更多
  8. SNIPER(ABL)-062

    Catalog No. A18567
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    ABL inhibitor
    SNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein. 了解更多
  9. Dasatinib Monohydrate

    Catalog No. A16320
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    Dasatinib Monohydrate是一种新型,有效且多靶点的抑制剂,靶向Abl,Src和c-Kit,IC50分别<1 nM,0.8 nM和79 nM。 了解更多
  10. ON 146040

    Catalog No. A16266
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    dual PI3K and BCR-ABL 抑制剂
    ON 146040是第一个靶向STAT3和STAT5途径的PI3K和BCR-ABL双重抑制剂;抑制PI3Kα/δ同工型,IC50为14/20 nM。 了解更多
  11. Lyn-IN-1

    Catalog No. A16265
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    dual Bcr-Abl/Lyn 抑制剂
    Lyn-IN-1是一种有效的选择性Bcr-Abl/Lyn双重抑制剂,摘自专利WO2014169128A1。 了解更多
  12. DPH

    Catalog No. A11379
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    c-ABL activitor
    DPH是一种有效的细胞渗透性c-Abl激活剂,在刺激c-Abl激活中显示出强大的酶和细胞活性。 了解更多
  13. GZD824 Dimesylate

    Catalog No. A15849
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    Bcr-Abl 抑制剂
    GZD824 Dimesylate是Bcr-Abl(WT)和Bcr-Abl(T315I)的新型生物可用Bcr-Abl抑制剂,IC50分别为0.34 nM和0.68 nM。 了解更多
  14. GNF-7

    Catalog No. A15887
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    Bcr-Abl 抑制剂
    GNF-7是一种有效的II型激酶Bcr-Abl抑制剂,对于M351T,T315I,E255 V,G250E和c-Abl,IC50分别<5 nM,61 nM,122 nM,136 nM和133 nM。 了解更多
  15. Flumatinib mesylate

    Catalog No. A13530
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    c-Abl/c-Kit/PDGRFβ 抑制剂
    Flumatinib mesylate以时间和剂量依赖性的方式降低U266细胞中C-MYC,HIF-1a和VEGF的表达,因此甲磺酸氟马替尼可能成为MM治疗的新药。 了解更多
  16. Imatinib (Gleevec)

    Catalog No. A10259
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    PDGFR 抑制剂
    Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。 了解更多
  17. Saracatinib (AZD0530)

    Catalog No. A10108
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    Src/Abl 抑制剂
    Saracatinib (AZD0530)是一种高选择性,双特异性Src/Abl激酶抑制剂,对c-Src和Abl激酶的IC50分别为2.7和30 nM。 了解更多
  18. AT9283

    Catalog No. A10095
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    Aurora/JAK 抑制剂
    AT9283抑制极光激酶A和B,并靶向与骨髓细胞增殖相关的其他酪氨酸和丝氨酸/苏氨酸激酶。 了解更多
  19. AP24534 (Ponatinib)

    Catalog No. A10080
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    BCR-ABL 抑制剂
    AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。 了解更多
  20. Danusertib (PHA-739358)

    Catalog No. A10715
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    Aurora 抑制剂
    Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂,在无细胞分析中的IC50为13 nM/79nM/61 nM,对Abl,TrkA,c-RET和FGFR1以及更低的浓度具有中等效力 对Lck,VEGFR2/3,c-Kit,CDK2等有效。 了解更多
  21. Bafetinib (INNO-406)

    Catalog No. A10119
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    Bcr-Abl 抑制剂
    Bafetinib (INNO-406)是一种双重Bcr-Abl/Lyn酪氨酸激酶抑制剂。 了解更多
  22. Dasatinib (BMS-354825)

    Catalog No. A10290
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    Abl-Src 抑制剂
    Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL,Src,c-Kit,ephrin受体和其他几种酪氨酸激酶,但不是erbB激酶,例如EGFR或Her2。 了解更多
  23. Nilotinib (AMN-107)

    Catalog No. A10644
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    Bcr-Abl 抑制剂
    Nilotinib (AMN-107)是一种Bcr-Abl抑制剂,IC50小于30 nM。 了解更多
  24. DCC-2036 (Rebastinib)

    Catalog No. A11200
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    Bcr-Abl 抑制剂
    DCC-2036 (Rebastinib)是一种Bcr-Abl抑制剂,作用于Abl1(WT)和Abl1(T315I),IC50分别为0.8 nM和4 nM,也抑制SRC, LYN, FGR, HCK, KDR, FLT3,和Tie-2,对c-Kit具有低的抑制活性。 了解更多
  25. Imatinib Mesylate

    Catalog No. A10468
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    Bcr-Abl 抑制剂
    Imatinib mesylate是一种选择性酪氨酸激酶抑制剂,通过抑制KIT信号转导途径,在治疗胃肠间质瘤中诱导了持续的客观反应。 了解更多
  26. NVP-BHG712

    Catalog No. A10661
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    EphB4 抑制剂
    NVP-BHG712是EphB4激酶的选择性抑制剂,在体外对EphB4的选择性超过40多种其他激酶(包括FGFR3)。 了解更多
  27. WP1130 (Degrasyn)

    Catalog No. A10988
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    DUB/Bcr/ABL 抑制剂
    WP1130 (Degrasyn)是一种新型的选择性小分子去泛素酶抑制剂和Bcr/Abl破坏途径激活剂,可特异性和快速下调野生型和突变型Bcr/Abl蛋白,而不会影响慢性粒细胞性白血病(CML)中的bcr/abl基因表达细胞。 了解更多
  28. KW-2449

    Catalog No. A10508
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    FLT3/FGFR/Bcr-Abl/Aurora 抑制剂
    KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。 了解更多
  29. GZD824

    Catalog No. A16264
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    Bcr-Abl 抑制剂
    GZD824是一种新型的口服生物利用型抑制剂,可抵抗包括T315I在内的各种Bcr-Abl突变体。 了解更多
  30. Flumatinib

    Catalog No. A16258
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    multi-kinase 抑制剂
    Flumatinib是一种多激酶抑制剂,对c-Abl,PDGFRbeta和c-Kit的IC50值分别为1.2 nM,307.6 nM和2662 nM。 了解更多
  31. PP121

    Catalog No. A11207
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    PI3K 抑制剂
    PP121是一种作用于PDGFR,Hck,mTOR,VEGFR2,Src和Abl的多靶点抑制剂,IC50分别为2 nM,8 nM,10 nM,12 nM,14 nM和18 nM,也抑制DNA-PK,IC50为60 nM。 了解更多
  32. Radotinib (IY-5511)

    Catalog No. A13029
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    Bcr-Abl tyrosine 抑制剂?
    Radotinib是一种新型的选择性Bcl-Abl酪氨酸激酶抑制剂。 了解更多
  33. AST 487

    Catalog No. A15003
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    RET kinase 抑制剂
    AST487是Ret激酶抑制剂/FLT3抑制剂,对Ret的IC50为0.88 uM。 了解更多
  34. Nilotinib monohydrochloride monohydrate

    Catalog No. A15186
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    Bcr-Abl 抑制剂
    Nilotinib monohydrochloride monohydrate是一种Bcr-Abl抑制剂,IC50小于30 nM。 了解更多
  35. NRC-AN-019

    Catalog No. A13562
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    Bcr-Abl 抑制剂
    NRC-AN-019是Bcr-Abl蛋白-酪氨酸激酶的口服酪氨酸激酶抑制剂(TKI)。NRC-AN-019在抑制MDAMB231和HTB20/BT474细胞的血管生成潜力和增殖方面更有效。 了解更多
  36. GNF 2

    Catalog No. A11439
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    Bcr-Abl 抑制剂
    GNF 2是一种Bcr-abl抑制剂,在表达Bcr-abl的细胞中抑制增殖并诱导凋亡。 了解更多
  37. GNF-5

    Catalog No. A13237
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    Bcr-Abl 抑制剂
    GNF-5是BCR-ABL的选择性变构抑制剂。 了解更多
  38. PD173955

    Catalog No. A13120
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    Bcr-Abl 抑制剂
    PD-173955是src酪氨酸激酶抑制剂。PD173955抑制Bcr-Abl依赖的细胞生长。PD173955显示G(1)中的细胞周期停滞。PD173955在Bcr-Abl的激酶抑制测定中的IC(50)为1-2 nM,在细胞生长测定中,其抑制Bcr-Abl依赖性底物酪氨酸磷酸化。 PD173955抑制试剂盒配体依赖性c-kit自磷酸化(IC(50)=约25 nM)和试剂盒配体依赖性M07e细胞增殖(IC(50)= 40 nM),但对白介素3依赖性(IC (50)= 250 nM)或粒细胞巨噬细胞集落刺激因子(IC(50)= 1 microM)依赖性细胞生长。 了解更多
  39. XL-228

    Catalog No. A13069
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    IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂
    XL228是靶向IGF1R,AURORA激酶,FGFR1-3,ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂(IC50,f3 nmol/L),对ABL1(Ki,5 nmol/L)以及BCR-ABL1 T315I(Ki,1.4 nmol/L)激酶显示出有效的生化活性。 了解更多

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