TAM Receptor
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1561 | BMS-777607 | <1 mg/mL | 47 mg/mL | <1 mg/mL |
| S2841 | R428 (BGB324) | <1 mg/mL | 6 mg/mL | <1 mg/mL |
| S4001 | Cabozantinib malate (XL184) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7342 | UNC2250 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S7846 | TP-0903 | <1 mg/mL | 3 mg/mL | 1 mg/mL |
| S8696 | 2-D08 | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S7576 | UNC2025 | 100 mg/mL | 25 mg/mL | 8 mg/mL |
| S7638 | LDC1267 | <1 mg/mL | 100 mg/mL | 2 mg/mL |
| S7325 | UNC2881 | <1 mg/mL | 92 mg/mL | 5 mg/mL |
| S8570 | RXDX-106 (CEP-40783) | <1 mg/mL | 10 mg/mL | 2 mg/mL |
| S8404 | S49076 | <1 mg/mL | 87 mg/mL | <1 mg/mL |
| S8573 | Sitravatinib (MGCD516) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7754 | Gilteritinib (ASP2215) | <1 mg/mL | 100 mg/mL | 85 mg/mL |
| S7669 | NPS-1034 | <1 mg/mL | 100 mg/mL | 4 mg/mL |
特异性亚型抑制剂
- TAM Receptor抑制剂（14）
- 新TAM Receptor产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1561 |
BMS-777607BMS-777607是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。 |
Numbers of clonogenic cells from L3.6pl cells and CSCs＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%. |
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| S2841 |
R428 (BGB324)R428 (BGB324)是一种Axl抑制剂，IC50为14 nM，作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR， EGFR， HER2，和PDGFRβ(高100倍以上)高。 |
Cetuximab-resistant cells are sensitive to therapeutic blockade of AXL activity with the AXL TKI R428. Cells were treated with vehicle (-) or indicated doses of R428 for 24 hours before harvesting whole-cell lysate and immunoblotting for the indicated proteins. α-Tubulin was used as a loading control.
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| S4001 |
Cabozantinib malate (XL184)Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐，是有效的VEGFR2抑制剂，IC50为0.035 nM，也抑制c-Met， Ret， Kit， Flt-1/3/4， Tie2和AXL，无细胞试验中IC50分别为1.3 nM， 4 nM， 4.6 nM， 12 nM/11.3 nM/6 nM， 14.3 nM和7 nM。 |
Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
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| S7342 |
UNC2250UNC2250是强效的选择性Mer抑制剂，IC50为1.7 nM，比高相关性的酶Axl/Tyro3选择性高了160和60倍。 |
a-c Concentration of secreted IL-1β, IL-8 and CCL2 in THP-1 macrophages treated with or without recombinant human IL-37 (rhIL-37) for 3 h, followed by incubation for 1 h with or without Mertk inhibitor and then incubated with lipopolysaccharide (LPS) or MSU separately for a further 18 h; *P < 0.05. d Different dosage of rhIL-37 was given preventively or therapeutically with or without Mertk inhibitor intervention in mice with gouty arthritis, and foot thickness was evaluated; *P < 0.05. e, f Histopathological analysis by H&E staining in a joint from the group treated with rhIL-37 treatment and Mertk inhibitor intervention (×100 original magnification (e) and × 200 original magnification (f); arrow inflammation in soft tissue and joint space.
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| S7846 |
TP-0903TP-0903是一种有效的选择性 AXL 抑制剂，IC50 为 27 nM。 |
Phosphorylation of Axl was analyzed by Western blotting of whole cell lysates using different antibodies. GAPDH was used as an internal control. H1299 cells were stimulated for 15 min with 400 nM recombinant human Gas6 (rGas6). H1299 cells were treated with or without TP-0903 (0.2 µmol/L) for 24 h.
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| S8696New |
2-D082-D08是一种具有细胞透性的蛋白类泛素化（protein sumoylation）抑制剂。它还能抑制Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR和PI3Kα，IC50分别为0.49, 3.9, 5.3, 9.8, 11, 11, 17和35 nM。 |
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| S7576 |
UNC2025UNC2025是一种有效且口服生物可利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM 和 0.8 nM，选择性比作用于Axl和 Tyro3大约高20倍。 |
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| S7638 |
LDC1267LDC1267是一种高选择性的TAM kinase抑制剂，对 Mer，Tyro3，和 Axl的IC50分别为<5 nM，8 nM，和 29 nM。对Met，Aurora B，Lck，Src，和 CDK8的活性较低。 |
Time- and dose-dependent effects of LDC1267 in RSC96 cells.
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| S7325 |
UNC2881UNC2881 是一种特异性的Mer tyrosine kinase抑制剂，IC50为 4.3 nM, 其选择性分别超过Axl和Tyro3的选择性 83倍，58倍。 |
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| S8570 |
RXDX-106 (CEP-40783)RXDX-106 (CEP-40783)是一种可口服的、有效的、选择性的TAM(TYRO3, AXL, MER)/MET抑制剂，在肽段磷酸化实验中具有较低的纳摩尔级别生化活性；在体外激酶结合试验中具有慢速的解离率（T1/2 >120 min）。 |
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| S8404 |
S49076S49076是一种新型的、有效的MET, AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。 |
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| S8573 |
Sitravatinib (MGCD516)Sitravatinib (MGCD516)是一种新型的、靶向多种参与调节S180肉瘤细胞生长的RTKs的小分子抑制剂，包括c-Kit, PDGFRβ, PDGFRα, c-Met和Axl。 |
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| S7754 |
Gilteritinib (ASP2215)Gilteritinib(ASP2215)是小分子FLT3/AXL抑制剂，对FLT3和AXL的IC50值为0.29 nM和0.73 nM。其抑制c-KIT的IC50值约为抑制FLT3的800倍。 |
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| S7669 |
NPS-1034NPS-1034是一种双Met/Axl抑制剂，IC50分别为48 nM和10.3 nM。 |
