SU 5402
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
| Cell experiment:[1] | |
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Cell lines |
Human myeloma cell line KMS11 |
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Reaction Conditions |
10 μmol/l SU 5402 for 72 h incubation |
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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] | |
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Animal models |
BALB/c mice with pre-B-TD cells injected subcutaneously into both flanks |
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Dosage form |
300 ng/kg Administered by either intraperitoneal injection or direct injection of one of the two tumors |
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Applications |
SU 5402 treatment (300 ng/kg) substantially decreased the level of activated ERK1/2 in pre-B-TD cells in vivo. |
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Note |
The technical data provided above is for reference only. |
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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. |
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质量控制和MSDS
- 批次:
化学结构
