Tyrosine Kinase

c-Kit-IN-3 (D-tartrate) (Compound 18) 是一种有效的 c-KIT kinase 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的IC50为 8 nM)，具有很高的生物利用度。

c-Kit-IN-3 hydrochloride (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的 IC50 为 8 nM)，具有很高的生物利用度。

Ensulizole (PBSA), a water soluble sunscreen ingredient, is a sulfonated UV absorber which is characterized by intense UVB and partial UVA absorption. Ensulizole can damage the DNA through the generation of reactive oxygen species (ROS) upon UV or sunlight irradiation.

GNF4877是 DYRK1A 和 GSK3β 的有效抑制剂，IC50 值分别为 6 nM 和 16 nM，可导致 NFATc 核输出受阻并增加 β 细胞增殖 (对小鼠 β (R7T1) 细胞的 EC50 值为 0.66 μM)。

IRAK4-IN-4 (compound 15) is an inhibitor of interleukin-1 receptor–associated kinase 4 (IRAK4) and cyclic GMP-AMP synthase (cGAS) with IC50 of 2.8 nM and 2.1 nM, respectively.

PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM).

An antagonist of PDGFRβ, FLT3, and c- Kit

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM.

Bozitinib (PLB-1001, CBT-101, APL-101, CBI-3103) is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) selectively inhibits MET-altered tumor cells in preclinical models.

S961 is a biosynthetic insulin receptor antagonist that inhibits cellular proliferation and colony formation in breast tumour cells.

TMP920 是一个高效、选择性的 RORγt 拮抗剂。TMP920 抑制 RORγt 结合 SRC1 肽的 IC50 值为 0.03 μM。

VU6015929 is a selective Discoidin Domain Receptor 1/2 (DDR1/2) inhibitor with IC50 of 4.67 nM and 7.39 nM for DDR1 and DDR2, respectively. VU6015929 potently inhibits collagen-IV production.

Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively.

A dual inhibitor of CK2 and ERK8

Imatinib D8 (STI571 D8) 是 Imatinib (STI571) 的氘代物。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。

Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively.

3-Hydroxy Midostaurin (CGP 52421) 是 PKC412 的代谢产物，可有效抑制 FMS 样酪氨酸激酶 3 (FLT3) 自磷酸化，在培养基和血浆中的 IC50 分别为 132 nM 和 9.8 μM。与 PKC412 相比，3-Hydroxy Midostaurin 的选择性较低，但细胞毒性更高。

A multi-kinase inhibitor

An internal standard for the quantification of bosutinib

An internal standard for the quantification of pazopanib

A non-selective caspase inhibitor

An internal standard for the quantification of regorafenib

An internal standard for the quantification of lapatinib

A multi-kinase inhibitor