| CAS NO: | 215543-92-3 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 296.33 |
| Cas No. | 215543-92-3 |
| Formula | C17H16N2O3 |
| Synonyms | SU-5402; SU5402 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥14.8 mg/mL in DMSO |
| Chemical Name | 3-[4-methyl-2-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid |
| Canonical SMILES | CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50：作用于VEGFR2、FGFR1、PDGFRβ和EGFR的IC50值分别为0.02、0.03、0.51和>100 μM。
SU 5402是一种VEGF、FGF和PDGF受体酪氨酸激酶抑制剂。受体酪氨酸激酶已被确认为治疗包括癌症、炎性疾病和心血管疾病在内的人类疾病的治疗靶点。
体外：SU5402在体外能够抑制FGFR3磷酸化。依赖于FGFR3存活的B细胞特异性地对SU5402敏感。对11种人骨髓瘤细胞系进行研究，其中五个t(4;14)易位。SU5402治疗后，表达组成型活性突变体FGFR3的KMS11人类骨髓瘤细胞系，G0/G1期细胞增加了95％，凋亡细胞增加4-5倍。此外，SU5402治疗后，激活信号调节激酶1和激酶2以及转录3的信号激活子迅速下调。在带有野生型FGFR3的人骨髓瘤细胞系中，SU5402消除aFGF配体的刺激作用[1]。
体内：BALB/c小鼠接种同系pre-B-TD细胞，通过直接皮下或腹膜内注射给药300 ng/kg SU5402或载体治疗这些已建立的肿瘤。24小时后收集肿瘤，蛋白质印迹分析表明，在治疗组中，在采集的肿瘤中活化ERK1/2的水平降低[1]。
临床试验：N/A
参考文献：
[1] Paterson JL,Li Z,Wen XY,μMasih-Khan E,Chang H,Pollett JB,Trudel S,Stewart AK. Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma. Br J Haematol.2004 Mar;124(5):595-603.
| Cell experiment:[1] | |
Cell lines | Human myeloma cell line KMS11 |
Reaction Conditions | 10 μmol/l SU 5402 for 72 h incubation |
Applications | The KMS11 human myeloma cell line, which expresses constitutively active mutant FGFR3, displayed an 85% decrease in S-phase cells, a 95% increase in G0/G1 cells, and 4.5-fold increase in apoptotic cells after 72 h treatment with 10 μmol/l SU 5402. Activated extracellular signal-regulated kinases 1 and 2 and signal transducer and activator of transcription 3 were rapidly down-regulated after SU 5402 treatment. |
| Animal experiment:[1] | |
Animal models | BALB/c mice with pre-B-TD cells injected subcutaneously into both flanks |
Dosage form | 300 ng/kg Administered by either intraperitoneal injection or direct injection of one of the two tumors |
Applications | SU 5402 treatment (300 ng/kg) substantially decreased the level of activated ERK1/2 in pre-B-TD cellsin vivo. |
Note | The technical data provided above is for reference only. |
References: 1. Paterson JL, Li Z, Wen XY, et al. Preclinical studies of fibroblast growth factor receptor 3 as a therapeutic target in multiple myeloma. British Journal of Haematology, 2004, 124(5): 595-603. | |
m.cnreagent.com