TL02-59是一种选择性的 Src-家族激酶 Fgr 抑制剂,能够有效抑制 Src-家族其他成员如 Lyn 和 Hck。它在急性髓性白血病 (AML) 研究中显示出显著的抗增生活性。


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| 产品名称 | Fyn ↓ ↑ | Lck ↓ ↑ | Lyn ↓ ↑ | Src ↓ ↑ | Yes ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Saracatinib |
++
Fyn, IC50: 10 nM |
++++
LCK, IC50: <4 nM |
+++
Lyn, IC50: 5 nM |
++++
c-Src, IC50: 2.7 nM |
99%+ | ||||||||||||||
| SU6656 |
+
Fyn, IC50: 170 nM |
+
Lyn, IC50: 130 nM |
+
Src, IC50: 280 nM |
++
YES, IC50: 20 nM |
98% | ||||||||||||||
| PP1 |
+++
Fyn, IC50: 6 nM |
+++
LCK, IC50: 5 nM |
EGFR | 99%+ | |||||||||||||||
| PP2 |
+++
Fyn, IC50: 5 nM |
++++
LCK, IC50: 4 nM |
98% | ||||||||||||||||
| WH-4-023 |
++++
Lck, IC50: 2 nM |
+++
Src, IC50: 6 nM |
99%+ | ||||||||||||||||
| NVP-BHG 712 |
+
c-Src, IC50: 1.266 μM |
99%+ | |||||||||||||||||
| CCT196969 |
++
LCK, IC50: 0.02 μM |
+
Src, IC50: 0.03 μM |
98% | ||||||||||||||||
| MNS |
+
Src, IC50: 29.3 μM |
p97,Syk | 98% | ||||||||||||||||
| Tirbanibulin |
++
Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM |
99%+ | |||||||||||||||||
| PP121 |
++
Src, IC50: 14 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
| Bosutinib |
++++
Src, IC50: 1.2 nM |
99% | |||||||||||||||||
| Dasatinib monohydrate |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Quercetin | ✔ | PKC,Sirtuin | 95% | ||||||||||||||||
| Dasatinib |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Repotrectinib |
+++
Src, IC50: 5.3 nM |
99% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| Concentration | Treated Time | Description | References | |
| MOLM-14 | MOLM-14 | Evaluate the inhibitory effect of TL02-59 on MOLM-14 cell growth | ACS Chem Biol. 2018 Jun 15;13(6):1551-1559. | |
| MV4-11 | MV4-11 | Evaluate the inhibitory effect of TL02-59 on MV4-11 cell growth | ACS Chem Biol. 2018 Jun 15;13(6):1551-1559. | |
| C57BL/6 mesenchymal stem cells | C57BL/6 mesenchymal stem cells | TL02-59 significantly reduced the expression of pro-fibrotic genes (Tgf-beta, Col1a1, 3, 4, 5, 6) in target cells | Cell Death Discov. 2023 Jul 17;9(1):252. | |
| Mouse primary lung fibroblasts | Mouse primary lung fibroblasts | TL02-59 significantly reduced the release of pro-fibrotic chemokines (LIX, CXCL5, CCL5, CXCL2, CCL20, G-CSF, IGFBP-3) from radiation-induced senescent cells | Cell Death Discov. 2023 Jul 17;9(1):252. | |
| tdTOMp16+ bone marrow mesenchymal stem cells | tdTOMp16+ bone marrow mesenchymal stem cells | Inhibition of Fgr kinase activity, reduction of fibrosis biomarker expression | Cell Death Discov. 2021 Nov 12;7(1):349. |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 mice | Radiation-induced pulmonary fibrosis model | Oral gavage | 10 mg/kg | 3 times a week for 4 weeks | TL02-59 significantly reduced radiation-induced pulmonary fibrosis, decreased the expression of pro-fibrotic genes (Tgf-β, Ctgf, Collagen 1a1, Collagen 3, Collagen 4), and reduced the infiltration of CD11b+ macrophages into the lungs | Cell Death Discov. 2023 Jul 17;9(1):252. |
| Mice | MV4-11 AML cell xenograft model | Oral | 1 and 10 mg/kg | Once daily for three weeks | Evaluate the efficacy of TL02-59 in a mouse AML model | ACS Chem Biol. 2018 Jun 15;13(6):1551-1559. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.64mL 0.33mL 0.16mL |
8.20mL 1.64mL 0.82mL |
16.40mL 3.28mL 1.64mL |
|
| CAS号 | 1315330-17-6 |
| 分子式 | C32H34F3N5O4 |
| 分子量 | 609.64 |
| SMILES Code | O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(OC4=C5C=C(OC)C(OC)=CC5=NC=N4)=C3 |
| MDL No. | MFCD29991221 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(172.23 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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