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SU 5402
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SU 5402图片
CAS NO:215543-92-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
25mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt296.33
Cas No.215543-92-3
FormulaC17H16N2O3
SynonymsSU-5402; SU5402
Solubilityinsoluble in EtOH; insoluble in H2O; ≥14.8 mg/mL in DMSO
Chemical Name3-[4-methyl-2-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
Canonical SMILESCC1=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。

资料参考

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.

试验操作

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.