BIBF1120 (Vargatef)，CAS号:656247-17-5, 790241-30-4 ，目录号 S1010，VEGFR YZ剂，VEGFR inhibitors，美国Selleck现货供应_详细资料

产品信息

供应商：美国Selleck南京办事处数量：大量保质期：两年保存条件：零下二十摄氏度低温保存英文名： BIBF1120 (Vargatef) CAS号： 656247-17-5, 790241-30-4 规格： 5mg

信号转导通路:  受体酪氨酸激酶(RTK) >> VEGFR >> VEGFR YZ剂 >> BIBF1120 (Vargatef)
http://selleck.cn/bibf1120-S1010.html
技术数据:

分子量(MW): 539.62

化学式:
C₃₁H₃₃N₅O₄

溶解度: DMSO ≥6mg/mL   Water <1mg/mL   Ethanol ≥3mg/mL

纯度: 99%

稳定性: at -20℃ 2 years

CAS号: 656247-17-5, 790241-30-4 (methanesulfonate), 959761-73-0 (HCl)

生物活性

An indolinone derivative potently blocking VEGF receptor(VEGFR), PDGFR and FGFR kinase activity.^[1]
The cytoplasmic tyrosine kinase domain of VEGFR-2 (residues 797–1355 according to sequence deposited in databank SWISS-PROT P35 68) was cloned into pFastBac fused to GST and extracted. For all the other kinase assays, the entire cytoplasmic domains of the receptors ( from the end of the transmembrane to the COOH terminus) were cloned into pFastBac vector containing GST and assayed under standard conditions.
Extensive biochemical testing revealed a distinctive, narrow range of kinases that are inhibited by BIBF 1120 at pharmacologically relevant concentrations.The targeted kinases include all three VEGFRsubtypes (IC50=13–34 nmol/L), PDGFRa and PDGFRh (IC50=59 and 65 nmol/L),and FGFRtypes 1, 2, and 3 (IC50=69, 37, and 108 nmol/L,respectively).
BIBF 1120 inhibits mitogenactivated protein kinase and Akt signaling pathways in three cell types contributing to angiogenesis, endothelial cells, pericytes, and smooth muscle cells, resulting in inhibition of cell proliferation (EC50=10–80 nmol/L) and apoptosis.^[2]

参考文献

Drug resistance by evasion of antiangiogenic targeting of VEGF signaling in late-stage pancreatic islet tumors Oriol Casanovas,Daniel J. Hicklin,et al. CANCER CELL OCTOBER 2005;8:299-309

BIBF 1120: Triple Angiokinase Inhibitor with Sustained Receptor Blockade and Good Antitumor Efficacy Gerald J. Roth, Martin Krssak, et al. Cancer Res 2008;68:4774-4782

客户反馈数据

PBLs from CLL5 were treated with vehicles (0.1% ethanol and 0.005% DMSO), 106 M dexamethasone, 50 nM BIBF 1120, or both for 24 h. Cells were also treated with 0.1% ethanol or 106 M dexamethasone in the presence of either nonphosphorylated (control) EGQYEEIP or phosphorylated EGQY*EEIP H2O soluble peptides (200 nM) for 24 h.

Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (± SD) from 3 experiments.

Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in “Materials and Methods”. The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group

Effect of BIBF 1120 on the expression of ABCB1 in MDR cells. Hep G2/adr and MCF-7/adr cells were treated with BIBF 1120 at various concentrations for 48 h. a The mRNA level of ABCB1 was determined by RT-PCR as described in “Materials and Methods”; b Equal amounts of total cell lysates were loaded and detected by Western blot. A representative result is shown from at least three independent experiments

Effect of BIBF 1120 on blockade of AKT and ERK1/2 phosphorylation. Hep G2/adr and MCF-7/adr cells were treated with drugs for 24 h. Equal amount of protein was loaded for Western blot as described in “Materials and Methods”. All these experiments were repeated at leas thrice, and a representative experiment is shown in each pane

BIBF 1120 inhibition of verapamil-stimulated ABCB1 ATPase activity. ABCB1 ATPase assays were performed according to the instruction of Pgp-Glo™ Assay Systems. Each point represents the mean±SDs for triplated independent determinations

如果需要长期保存，请于零下二十度低温保存。

禁止用于人体及ZL！

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20 ° C ，抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

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温馨提示：不可用于临床ZL。

分子量(MW):	539.62
化学式:	C₃₁H₃₃N₅O₄
溶解度:	DMSO ≥6mg/mL Water <1mg/mL Ethanol ≥3mg/mL
纯度:	99%
稳定性:	at -20℃ 2 years
CAS号:	656247-17-5, 790241-30-4 (methanesulfonate), 959761-73-0 (HCl)

	PBLs from CLL5 were treated with vehicles (0.1% ethanol and 0.005% DMSO), 106 M dexamethasone, 50 nM BIBF 1120, or both for 24 h. Cells were also treated with 0.1% ethanol or 106 M dexamethasone in the presence of either nonphosphorylated (control) EGQYEEIP or phosphorylated EGQY*EEIP H2O soluble peptides (200 nM) for 24 h.
	Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (± SD) from 3 experiments.
	Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in “Materials and Methods”. The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group
	Effect of BIBF 1120 on the expression of ABCB1 in MDR cells. Hep G2/adr and MCF-7/adr cells were treated with BIBF 1120 at various concentrations for 48 h. a The mRNA level of ABCB1 was determined by RT-PCR as described in “Materials and Methods”; b Equal amounts of total cell lysates were loaded and detected by Western blot. A representative result is shown from at least three independent experiments
	Effect of BIBF 1120 on blockade of AKT and ERK1/2 phosphorylation. Hep G2/adr and MCF-7/adr cells were treated with drugs for 24 h. Equal amount of protein was loaded for Western blot as described in “Materials and Methods”. All these experiments were repeated at leas thrice, and a representative experiment is shown in each pane
	BIBF 1120 inhibition of verapamil-stimulated ABCB1 ATPase activity. ABCB1 ATPase assays were performed according to the instruction of Pgp-Glo™ Assay Systems. Each point represents the mean±SDs for triplated independent determinations

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BIBF1120 (Vargatef)，CAS号:656247-17-5, 790241-30-4 ， 目录号 S1010，VEGFR YZ剂，VEGFR inhibitors，美国Selleck现货供应

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BIBF1120 (Vargatef)，CAS号:656247-17-5, 790241-30-4 ，目录号 S1010，VEGFR YZ剂，VEGFR inhibitors，美国Selleck现货供应