货号:A161457
同义名:
KX-01; KX2-391
Tirbanibulin 是一种 Src 激酶抑制剂,对多种癌细胞系的 GI₅₀ 范围为 9–60 nM,可用于细胞周期调控及 Src 通路机制研究。


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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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. |
| Concentration | Treated Time | Description | References | |
| MDA-MB-468 | 10-250 nM | 48 h | KX-01 inhibited the growth of MDA-MB-468 cells. | Mol Cancer Ther. 2012 Sep;11(9):1936-47. |
| MDA-MB-231 | 10-250 nM | 48 h | KX-01 inhibited the growth of MDA-MB-231 cells. | Mol Cancer Ther. 2012 Sep;11(9):1936-47. |
| MDA-MB-157 | 10-250 nM | 48 h | KX-01 inhibited the growth of MDA-MB-157 cells. | Mol Cancer Ther. 2012 Sep;11(9):1936-47. |
| H460 cells | 100 nM | 16 h | KXO1 induced G2/M phase cell cycle arrest | J Biol Chem. 2019 Nov 29;294(48):18099-18108. |
| HepG2 cells | 50 nM | 16 h | KXO1 induced G2/M phase cell cycle arrest | J Biol Chem. 2019 Nov 29;294(48):18099-18108. |
| Ba/F3 cells | 1 µM | 1 hour | Evaluate the inhibitory effect of KX2-391 on FLT3-ITD cells | J Hematol Oncol. 2021 Jul 3;14(1):105. |
| Pa16C | 80 nM | 24 h | To evaluate the effect of Tirbanibulin on MYC protein levels and phosphorylation | Cell Rep. 2021 Jun 29;35(13):109291. |
| human monocyte-derived macrophages (HMDM) | 0.33 μM | 15 h | Tirbanibulin significantly enhanced the killing of VRE by HMDM. | ACS Infect Dis. 2024 May 10;10(5):1725-1738. |
| RAW264.7 macrophages | 0.33 μM | 15 h | Tirbanibulin stimulated macrophage killing of bacteria, significantly reducing intracellular VRE CFU. | ACS Infect Dis. 2024 May 10;10(5):1725-1738. |
| HeLa cells | 30 nM | 16 h | KXO1 inhibited tubulin polymerization and induced G2/M phase cell cycle arrest | J Biol Chem. 2019 Nov 29;294(48):18099-18108. |
| HeLa cells | 12.5, 25, 50, 100 nM | 16 h | KXO1 induced G2/M phase cell cycle arrest, further confirming that KXO1 is a strong tubulin inhibitor. | J Biol Chem. 2019 Nov 29;294(48):18099-18108. |
| HeLa cells | 30 nM | 16 h | KXO1 inhibited tubulin polymerization, confirming that KXO1 is a strong tubulin depolymerization agent. | J Biol Chem. 2019 Nov 29;294(48):18099-18108. |
| Administration | Dosage | Frequency | Description | References | ||
| Mouse | Pancreatic cancer model | Oral | 15 mg/kg | Daily for 14 days | To evaluate the inhibitory effect of Tirbanibulin in combination with ERK inhibitor on pancreatic cancer growth | Cell Rep. 2021 Jun 29;35(13):109291. |
| Mice | Wound infection model | Intraperitoneal injection | 5 mg/kg | Single dose | Tirbanibulin significantly reduced VRE CFU in wounds, demonstrating its antibacterial efficacy in vivo. | ACS Infect Dis. 2024 May 10;10(5):1725-1738. |
| Mice | FLT3-ITD-F691L leukemia model | Oral | 10 mg/kg | Once daily for 10 days | Evaluate the therapeutic effect of KX2-391 on FLT3-ITD-F691L leukemia model, significantly prolonging survival | J Hematol Oncol. 2021 Jul 3;14(1):105. |
| BALB/c nude mice | Lung and liver metastasis models | Oral | 15 mg/kg | Daily for 9 weeks | To evaluate the inhibitory effects of combined therapy with BLU-554 and KX2-391 on ELF4-mediated CRC metastasis. The results showed that combined treatment significantly inhibited lung and liver metastasis and prolonged the survival of mice. | Theranostics. 2023 Feb 22;13(4):1401-1418 |
| Nude mice | MDA-MB-231 tumor xenograft model | Oral | 1 mg/kg and 5 mg/kg | Twice daily for 28 days | KX-01 significantly inhibited the growth of MDA-MB-231 tumors. | Mol Cancer Ther. 2012 Sep;11(9):1936-47. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.59mL 2.32mL 1.16mL |
23.17mL 4.63mL 2.32mL |
|
| CAS号 | 897016-82-9 |
| 分子式 | C26H29N3O3 |
| 分子量 | 431.53 |
| SMILES Code | O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2 |
| MDL No. | MFCD18633218 |
| 别名 | KX-01; KX2-391 |
| 运输 | 蓝冰 |
| InChI Key | HUNGUWOZPQBXGX-UHFFFAOYSA-N |
| Pubchem ID | 23635314 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 40 mg/mL(92.69 mM),配合低频超声助溶,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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