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FLT3

Inhibitory Selectivity

Catalog No.Inhibitor Name FLT3Other
A10996Cabozantinib
**
VEGFR2/KDR,c-Met,Kit
A10027Quizartinib
***
A11411Dovitinib
****
c-Kit,VEGFR3/FLT4,FGFR1
A10610Amuvatinib
*
c-Kit (D816H),PDGFRα (V561D)
A10887Tandutinib
*
c-Kit,PDGFRβ,CSF-1R
A11180TG101209
*
JAK2,RET,JAK3
A10508KW-2449
****
Abl (T315I),Abl,FGFR1
A10352ENMD-2076
***
RET,Aurora A,VEGFR3/FLT4
A10198Dovitinib Dilactic Acid
****
c-Kit,FGFR1,VEGFR3/FLT4
A12694Pacritinib
**
JAK2 (V617F),JAK2,TYK2
A12427TCS 359
*
A10352ENMD-2076 L-(*)-Tartaric acid
RET,Aurora A,VEGFR3/FLT4
A15904UNC2025
****
Mer
A14025AMG 925
****
CDK4,CDK1
A14214G-749
****
Mer,Aurora B,RET
A14156AZD2932
PDGFRβ,VEGFR-2,c-Kit
A10769R406
Syk
A12419Go6976
JAK2,PKCα,PKCβ1
A11962TG-02 (SB1317)
*
CDK2, JAK2
A14411Gilteritinib (ASP2215)
****
Axl
A15003AST 487
Ret, c-Kit, KDR, c-Abl
A15520Pexidartinib (PLX3397)
*
Kit, CSF-1R
A15548SU5614
A16248BPR1J-097
**

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.

42 个项目

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  1. SB1317 (TG02)
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    SB1317 (TG02)

    Catalog No. A13454
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    CDK/JAK2/FLT3 抑制剂
    SB1317是细胞周期蛋白依赖性激酶（CDKs）、类FMS酪氨酸激酶-3（FLT3）和Janus激酶2（JAK2）的有效抑制剂，CDK2、JAK2和FLT3的IC50值分别为13nM、56nM和73nM。 了解更多
  2. MRX-2843
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    MRX-2843

    Catalog No. A16958
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    MERTK and FLT3 抑制剂
    MRX-2843是MERTK和FLT3的口服小分子抑制剂。 了解更多
  3. BSc5371
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    BSc5371

    Catalog No. A19465
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    FLT3 inhibitor
    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. 了解更多
  4. TG-101348 (Fedratinib, SAR302503)
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    TG-101348 (Fedratinib, SAR302503)

    Catalog No. A11082
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    JAK2/FLT3 抑制剂
    TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型，ATP竞争性和选择性抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。 了解更多
  5. PROTAC FLT-3 degrader 1
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    PROTAC FLT-3 degrader 1

    Catalog No. A18682
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    FLT-3 ITD degrader
    PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction. 了解更多
  6. FLT3-IN-4
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    FLT3-IN-4

    Catalog No. A18509
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    FLT3 inhibitor
    FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia. 了解更多
  7. FN-1501
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    FN-1501

    Catalog No. A13559
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    FLT3/CDK inhibitor
    FN-1501 is a potent inhibitor of FLT3 and 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. FN-1501 has anticancer activity. 了解更多
  8. Gilteritinib hemifumarate
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    Gilteritinib hemifumarate

    Catalog No. A18235
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    FLT3/AXL inhibitor
    Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively. 了解更多
  9. CCT241736
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    CCT241736

    Catalog No. A21097
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    dual FLT3/Aurora kinase inhibitor
    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor. 了解更多
  10. FLT3-IN-3
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    FLT3-IN-3

    Catalog No. A20172
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    FLT3 inhibitor
    FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively. 了解更多
  11. R406 (Tamatinib)
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    R406 (Tamatinib)

    Catalog No. A10770
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    Syk 抑制剂
    R406 (Tamatinib)是一种口服酪氨酸激酶抑制剂，IC50为41 nM。对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。 了解更多
  12. TAK-659
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    TAK-659

    Catalog No. A20450
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    SYK/FLT3 inhibitor
    TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. 了解更多
  13. 5'-Fluoroindirubinoxime
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    5'-Fluoroindirubinoxime

    Catalog No. A22692
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    FLT3 inhibitor
    5'-Fluoroindirubinoxime (5??-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM. 了解更多
  14. HM-43239
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    HM-43239

    Catalog No. A20826
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    FLT3 inhibitor
    HM-43239 is a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations 了解更多
  15. FLT3-IN-2
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    FLT3-IN-2

    Catalog No. A16250
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    FLT3 抑制剂
    FLT3-IN-2是有效的FLT3抑制剂。 了解更多
  16. FLT3-IN-1
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    FLT3-IN-1

    Catalog No. A16249
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    FLT3 抑制剂
    FLT3-IN-1是一种新型的有效选择性Flt3抑制剂，IC50为10 nM。抗表达FLT3-ITD的MV4-11细胞，IC50为6 nM。 了解更多
  17. BPR1J-097
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    BPR1J-097

    Catalog No. A16248
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    FLT3 抑制剂
    BPR1J-097是一种新颖的小分子FLT-3抑制剂，具有良好的体内抗肿瘤活性。 了解更多
  18. AC710 Mesylate
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    AC710 Mesylate

    Catalog No. A16246
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    FLT3/KIT/PDGFRα/PDGFRβ 抑制剂
    AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂，对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。 了解更多
  19. UNC-2025
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    UNC-2025

    Catalog No. A15904
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    Dual MER/FLT3 抑制剂
    UNC-2025是一种有效的且可生物利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM和0.8 nM，选择性是Axl和Tyro3的20倍。 了解更多
  20. SU5614
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    SU5614

    Catalog No. A15548
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    FLT3 抑制剂
    SU5614是有效的选择性FLT3抑制剂。SU5614恢复了FL依赖性细胞中FLT3配体（FL）的抗凋亡和增殖活性。 了解更多
  21. Pexidartinib (PLX3397)
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    Pexidartinib (PLX3397)

    Catalog No. A15520
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    CSF1/Kit/FLT3 抑制剂
    Pexidartinib (PLX3397)是KIT，CSF1R和FLT3的小分子酪氨酸激酶（RTK）抑制剂，具有潜在的抗肿瘤活性。 了解更多
  22. AST 487
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    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
  23. AC220 (Quizartinib)
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    AC220 (Quizartinib)

    Catalog No. A10027
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    FLT3 抑制剂
    AC220 (Quizartinib)是一种有效的选择性FLT3抑制剂，对于MC4-11和A375，IC50分别为0.56±0.3 nM和> 10 mM。 了解更多
  24. XL184 free base (Cabozantinib)
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    XL184 free base (Cabozantinib)

    Catalog No. A10996
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    VEGFR 抑制剂
    XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶（特别是MET和VEGFR2）的小分子。 了解更多
  25. R406 besylate
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    R406 besylate

    Catalog No. A10769
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    Syk 抑制剂
    R406 besylate是一种口服酪氨酸激酶抑制剂，IC50为41 nM。对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。 了解更多
  26. Dovitinib (TKI-258)
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    Dovitinib (TKI-258)

    Catalog No. A11411
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    RTK 抑制剂
    Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。 了解更多
  27. MP470 (MP-470, Amuvatinib)
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    MP470 (MP-470, Amuvatinib)

    Catalog No. A10610
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    RTK 抑制剂
    MP470 (MP-470,Amuvatinib)是c-Kit/PDGFR酪氨酸激酶抑制剂。 了解更多
  28. Tandutinib (MLN518)
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    Tandutinib (MLN518)

    Catalog No. A10887
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    FLT3 抑制剂
    Tandutinib (MLN518)是一种有效的FLT3抑制剂，c-KIT和PDGF受体酪氨酸激酶的自磷酸化，从而抑制细胞增殖并诱导细胞凋亡。 了解更多
  29. Crenolanib (CP-868596)
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    Crenolanib (CP-868596)

    Catalog No. A11052
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    PDGFR/FLT3 抑制剂
    Crenolanib (CP-868596)是口服生物可用的PDGFR酪氨酸激酶的选择性小分子抑制剂，在皮摩尔浓度下抑制PDGFRA和PDGFRB。 了解更多
  30. ENMD-2076
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    ENMD-2076

    Catalog No. A10352
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    Aurora A / FLT3 抑制剂
    ENMD-2076具有针对Aurora A和Flt3的选择性活性，IC50为14 nM和1.86 nM，对Aurora A的选择性是Aurora B的25倍，对VEGFR2/KDR和VEGFR3，FGFR1和FGFR2和PDGFRα的作用较小。阶段2。 了解更多
  31. KW-2449
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    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
  32. TG101209
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    TG101209

    Catalog No. A11180
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    JAK2 抑制剂
    TG101209是一种新型的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。在多发性骨髓瘤中具有显着的体外活性，并且对CD45+骨髓瘤细胞显示出优先的细胞毒性。 了解更多
  33. Dovitinib Dilactic acid (TKI258 Dilactic acid)
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    Dovitinib Dilactic acid (TKI258 Dilactic acid)

    Catalog No. A10198
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    RTK 抑制剂
    Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。 了解更多
  34. MK-2461
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    MK-2461

    Catalog No. A11753
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    c-Met 抑制剂
    MK-2461是一种新型的多靶点激酶抑制剂，优先抑制活化的c-Met受体。 了解更多
  35. Go 6976
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    Go 6976

    Catalog No. A12419
    PKC 抑制剂
    Go6976是一种有效的PKC抑制剂，对PKC（大鼠脑），PKCα和PKCβ1的IC50分别为7.9 nM，2.3 nM和6.2 nM。也是JAK2和Flt3的有效抑制剂。 了解更多
  36. TCS 359
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    TCS 359

    Catalog No. A12427
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    FLT3 抑制剂
    TCS 359是一种有效的FLT3受体酪氨酸激酶抑制剂（IC50 = 42 nM），对多种其他激酶具有选择性。 了解更多
  37. Pacritinib (SB1518)
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    Pacritinib (SB1518)

    Catalog No. A12694
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    JAK2/FLT3 抑制剂
    Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。 了解更多
  38. AZD 2932
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    AZD 2932

    Catalog No. A14156
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    mutil-targeted protein tyrosine kinase 抑制剂
    AZD2932是一种有效且靶向多用途的蛋白酪氨酸激酶抑制剂，对VEGFR-2，PDGFRβ，Flt-3和c-Kit的IC50分别为8 nM，4 nM，7 nM和9 nM。 了解更多
  39. TG-02 (SB1317)
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    TG-02 (SB1317)

    Catalog No. A11962
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    FLT3 抑制剂
    TG-02 (SB1317)是一种新型的小分子有效CDK/JAK2/FLT3抑制剂。 了解更多
  40. G-749
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    G-749

    Catalog No. A14214
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    FLT3 抑制剂
    G-749是一种新型有效的FLT3抑制剂，对于FLT3（WT），FLT3（D835Y）的IC50为0.4 nM，0.6 nM和1 nM。 了解更多
  41. Gilteritinib (ASP2215)
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    Gilteritinib (ASP2215)

    Catalog No. A14411
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    FLT3/Axl 抑制剂
    Gilteritinib (ASP2215)是一种有效的FLT3/AXL抑制剂，对具有AML突变或FLT3-ITD和FLT3-D835的AML具有有效的抗白血病活性。 了解更多
  42. AMG-925
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    AMG-925

    Catalog No. A14025
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    Dual FLT3/CDK4 抑制剂
    AMG-925是一种有效，选择性和生物利用性的FLT3/细胞周期蛋白依赖性激酶4（CDK4）双激酶抑制剂。 了解更多

42 个项目

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作用机制
  1. Inhibitor (抑制剂) (41)
  2. Degrader (降解剂) (1)
靶点
  1. Abl (1)
  2. Aurora A (2)
  3. Axl (1)
  4. CDK (2)
  5. CDK4 (1)
  6. CSF1R (4)
  7. FGFR1 (3)
  8. FGFR3 (2)
  9. FLT3 (25)
  10. JAK2 (7)
  11. Kit (5)
  12. Mer (1)
  13. PDGFRα (2)
  14. PDGFRβ (5)
  15. PKCα (1)
  16. PKCβ (1)
  17. RET (2)
  18. Src (1)
  19. Syk (1)
  20. VEGFR1 (FLT1) (2)
  21. VEGFR2 (FLK1) (2)
  22. VEGFR3 (FLT4) (2)
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