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Cat. No. Product Name Target Signaling Pathways
T4332 c-Kit-IN-1

PDGFR inhibitor 1,DCC-2618

c-Met/HGFR; c-Kit Tyrosine Kinase/Adaptors
c-Kit-IN-1 (DCC-2618) 是c-Kitc-Met 抑制剂(IC50<200 nM)。
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、FGFR1c-Fms 的IC50分别为10、30、47、84、74、140和146 nM。
T2668 JNK-IN-8

JNK Inhibitor XVI

JNK; c-Kit MAPK; Tyrosine Kinase/Adaptors
JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的JNK 抑制剂,抑制JNK1、JNK2和JNK3,IC50分别为 4.7、18.7 和 1 nM。
T4349 Sitravatinib

MG516,MGCD516

Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor Angiogenesis; Tyrosine Kinase/Adaptors
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。
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-1c-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).
T10645 c-Fms-IN-6

c-Fms Tyrosine Kinase/Adaptors
c-Fms-IN-6 is a potent inhibitor of c-FMS (IC50 ≤10 nM for unphosphorylated c-FMS) and also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50: > 1 μM).
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.
T61313 Antitumor agent-70

Antitumor agent-70 (compound 8b) is a highly potent multi-targeted kinase inhibitor, particularly targeting c-Kit. It demonstrates remarkable anti-tumor activity and the ability to induce cell apoptosis. This compound also exhibits strong inhibition of multiple myeloma, with an IC 50 value of 0.12 μM. Therefore, Antitumor agent-70 holds great potential as an effective therapy for combating cancer, especially in cases involving c-Kit. [1]
T9665 Esuberaprost Sodium

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].
T82393 FLT3/CHK1-IN-1

FLT3/CHK-IN-1Compound 18)为FLT3/CHK1双重抑制剂,其对c-KIT的选择性超1700倍,同时显著降低对hERG的亲和力,IC50为58.4 μM。在MV-4-11细胞接种小鼠异种移植模型中有效抑制肿瘤生长。
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。
T78305 Briquilimab

JSP-191

Briquilimab (JSP-191) 是针对 CD117 (c-Kit) 的无毒人源化单克隆抗体,用于消耗造血干细胞 (HSC)。它被应用于重度联合免疫缺陷 (SCID) 治疗中,以清空宿主骨髓生态位,为供体造血干细胞移植及免疫重建创造条件。
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。
T81740 Multi-kinase-IN-6

Trk receptor Tyrosine Kinase/Adaptors
Multi-kinase-IN-6 (compound 10e) 是一种效能极高的多激酶抑制剂,具有对 TrkA、ALK2、c-KIT、EGFR、PIM1CK2α、CHK1CDK2 等多种酶的显著抑制作用。在 MCF7、HCT116 和 EKVX 癌细胞系上,其抗增殖活性突出,IC50 值分别达到 3.36 μM、1.40 μM 与 3.49 μM。此外,Multi-kinase-IN-6 能引起 MCF7 与 HCT116 细胞的细胞周期在 G1/S 期及 G1 期停滞,并有效诱导凋亡。
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、33、36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-1
Cat.No: T4332
Synonym: PDGFR inhibitor 1,DCC-2618
Target: c-Met/HGFR, c-Kit
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
JNK-IN-8
Cat.No: T2668
Synonym: JNK Inhibitor XVI
Target: JNK, c-Kit
Sitravatinib
Cat.No: T4349
Synonym: MG516,MGCD516
Target: Discoidin Domain Receptor (DDR), VEGFR, FLT, Trk receptor, TAM Receptor, c-Kit, Ephrin Receptor
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
c-Fms-IN-6
Cat.No: T10645
Synonym:
Target: c-Fms
NAMPT inhibitor-linker 1
Cat.No: T18477
Synonym:
Target: Others
Antitumor agent-70
Cat.No: T61313
Synonym:
Target:
Esuberaprost Sodium
Cat.No: T9665
Synonym:
Target:
FLT3/CHK1-IN-1
Cat.No: T82393
Synonym:
Target:
Multi-kinase-IN-2
Cat.No: T63967
Synonym:
Target:
Briquilimab
Cat.No: T78305
Synonym: JSP-191
Target:
Imatinib Impurity E
Cat.No: T73973
Synonym:
Target:
Multi-kinase-IN-6
Cat.No: T81740
Synonym:
Target: Trk receptor
CYY292
Cat.No: T83911
Synonym:
Target:
TargetMol Loading
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