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Cat. No. Product Name Target Signaling Pathways
T10651 c-Kit-IN-3

c-Kit Tyrosine Kinase/Adaptors
c-Kit-IN-3c-KIT 激酶的特异性抑制剂,对 c-Kit (wt) 和 c-Kit (T670I) 的 IC50 分别为 4 nM、8 nM。
T19222 c-Kit-IN-3 maleate

Others Others
c-Kit-IN-3 maleate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).
T19220 c-Kit-IN-3 hydrochloride

Others Others
c-Kit-IN-3 hydrochloride is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).
T19223 c-Kit-IN-3 tartrate

Others Others
c-Kit-IN-3 tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).
T19221 c-Kit-IN-3 L-tartrate

Others Others
c-Kit-IN-3 L-tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).
T19219 c-Kit-IN-3 D-tartrate

Others Others
c-Kit-IN-3 D-tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).
T2051 SKLB4771

FLT3-​IN-​1,FLT3-IN-1

FLT Angiogenesis; Tyrosine Kinase/Adaptors
SKLB4771 (FLT3-IN-1) 是一种新型的、高效的 Flt3 抑制剂 (IC50:10nM)。
T22256 c-Kit-IN-5-1

3-(2-Aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one,AMG-25,3-(2-aminoquinazolin-6-yl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]pyridin-2-one

c-Kit Tyrosine Kinase/Adaptors
c-Kit-IN-5-1 (AMG-25) 是一种新型的、高效的、选择性的 c-Kit 抑制剂。
T0097L Pazopanib

帕唑帕尼,GW786034

VEGFR; FGFR; PDGFR; c-Kit; Autophagy Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors
Pazopanib (GW786034) 是一种小分子抑制剂,可抑制多种具有潜在抗肿瘤活性的蛋白酪氨酸激酶。它抑制VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1和c-Fms 的IC50分别为10、30、47、84、74、140和146 nM。
T2500 Cediranib

AZD2171,NSC-732208,西地尼布

VEGFR; FLT; PDGFR; c-Kit; Autophagy Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors
Cediranib (AZD2171) 是一种可口服的高选择性VEGFR2抑制剂,对Flt1、KDR、Flt4、PDGFRα、PDGFRβ和c-Kit 的IC50值分别为小于1、小于3、5、5、36和 2nM。
T3211 Midostaurin

米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱

Others; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Others
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kitc-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。
T2624 OSI-930

OSI 930,噻尔非尼

Apoptosis; c-Fms; Raf; VEGFR; FLT; CSF-1R; Src; c-Kit Angiogenesis; Apoptosis; MAPK; Tyrosine Kinase/Adaptors
OSI-930 是 Kit,KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂,IC50分别为 80 nM,9 nM 和 15 nM。它具有抗肿瘤活性,靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1,c-Raf 和 Lck,并且对 PDGFRα/β,Flt-3和 Abl 具有较弱的抑制活性。
T10650 c-Kit-IN-2

c-Kit Tyrosine Kinase/Adaptors
c-Kit-IN-2 is a c-KIT inhibitor (IC50: 82 nM), shows superior antiproliferative activities against all the three GIST cell lines, GIST430, GIST882, and GIST48 (GI50s: 1, 3, and 2 nM).
T18477 NAMPT inhibitor-linker 1

Others Others
NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.
T63967 Multi-kinase-IN-2

Multi-kinase-IN-2 是口服具有活力的血管激酶 (angiokinase) 抑制剂。Multi-kinase-IN-2 能够显著抑制血管激酶的活性,如 VEGFR-1/2/3、PDGFRα/β、FGFR-1、LYN 和 c-KIT 激酶。Multi-kinase-IN-2 能够明显减弱 AKT 和 ERK 蛋白的磷酸化,并可诱导细胞凋亡 (apoptosis),具有抗癌作用。
T73973 Imatinib Impurity E

Imatinib Impurity E 是 Imatinib 的杂质。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂,可选择性抑制 BCR/ABL,v-Abl,PDGFR,c-kit 激酶活性。Imatinib (STI571) 靠近 ATP 结合位点结合,将其锁定在封闭或自我抑制的构象中,因此半竞争性抑制蛋白质的酶活性。Imatinib 还抑制 SARS-CoV 和MERS-CoV。
T83911 CYY292

CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、3336和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。

化合物

c-Kit-IN-3
Cat.No: T10651
Synonym:
Target: c-Kit
c-Kit-IN-3 maleate
Cat.No: T19222
Synonym:
Target: Others
c-Kit-IN-3 hydrochloride
Cat.No: T19220
Synonym:
Target: Others
c-Kit-IN-3 tartrate
Cat.No: T19223
Synonym:
Target: Others
c-Kit-IN-3 L-tartrate
Cat.No: T19221
Synonym:
Target: Others
c-Kit-IN-3 D-tartrate
Cat.No: T19219
Synonym:
Target: Others
SKLB4771
Cat.No: T2051
Synonym: FLT3-​IN-​1,FLT3-IN-1
Target: FLT
c-Kit-IN-5-1
Cat.No: T22256
Synonym: 3-(2-Aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one,AMG-25,3-(2-aminoquinazolin-6-yl)-4-methyl-1-[4-(1,3-oxazol-2-yl)phenyl]pyridin-2-one
Target: c-Kit
Pazopanib
Cat.No: T0097L
Synonym: 帕唑帕尼,GW786034
Target: VEGFR, FGFR, PDGFR, c-Kit, Autophagy
Cediranib
Cat.No: T2500
Synonym: AZD2171,NSC-732208,西地尼布
Target: VEGFR, FLT, PDGFR, c-Kit, Autophagy
Midostaurin
Cat.No: T3211
Synonym: 米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱
Target: Others, PKC
OSI-930
Cat.No: T2624
Synonym: OSI 930,噻尔非尼
Target: Apoptosis, c-Fms, Raf, VEGFR, FLT, CSF-1R, Src, c-Kit
c-Kit-IN-2
Cat.No: T10650
Synonym:
Target: c-Kit
NAMPT inhibitor-linker 1
Cat.No: T18477
Synonym:
Target: Others
Multi-kinase-IN-2
Cat.No: T63967
Synonym:
Target:
Imatinib Impurity E
Cat.No: T73973
Synonym:
Target:
CYY292
Cat.No: T83911
Synonym:
Target:
TargetMol Loading
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