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  1. Protein Tyrosine Kinase/RTK
  2. PDGFR
  3. AG 1295

AG 1295 是一種選擇性血小板衍生生長因子受體 (PDGFR) 酪氨酸激酶抑制劑。AG1295 能抑制 PDGFR 的自磷酸化,對 EGF 受體的自磷酸化無效。

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AG 1295 Chemical Structure

AG 1295 Chemical Structure

CAS No. : 71897-07-9

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10 mM * 1 mL in DMSO ¥660
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查看 PDGFR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor[1][2][3][4].

IC50 & Target

PDGFR[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
MV4-11 IC50
2.2 μM
Compound: AG1295
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
[PMID: 32659083]
NIH3T3 IC50
0 μM
Compound: AG-1295
Antitumor activity measured by the inhibition of platelet-derived growth factor receptor autophosphorylation in intact Swiss 3T3 cells
Antitumor activity measured by the inhibition of platelet-derived growth factor receptor autophosphorylation in intact Swiss 3T3 cells
[PMID: 11855980]
SF-539 IC50
6.2 μM
Compound: 28
Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
[PMID: 23375090]
SF-539 IC50
6.2 μM
Compound: 22, AG-1295
Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA
Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA
[PMID: 22370340]
U-251 IC50
6.2 μM
Compound: 18, AG-1295
Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA
Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA
[PMID: 19748785]
體外研究
(In Vitro)

AG 1295 抑制 PDGFR 自磷酸化,膜自磷酸化測定和 Swiss 3T3 細(xì)胞的 IC50 分別為 0.3-0.5 μM 和 0.5-1 μM[1]。
AG1295 (10 μM、100 μM) 在體外顯著抑制 PDGF-AAPDGF-BB 刺激的兔結(jié)膜成纖維細(xì)胞生長[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Rabbit conjunctival fibroblasts cells
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 3 days
Result: Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB.
體內(nèi)研究
(In Vivo)

AG-1295 通過抑制 PDGFR-β 觸發(fā)的酪氨酸磷酸化來減少主動脈同種異體移植物血管病變中的新內(nèi)膜形成[3]。
AG1295 (12 mg/kg;腹腔注射;每天;14 或 21 天天) 顯著減少間質(zhì)纖維化,這已通過較小的天狼星紅染色區(qū)域和巨噬細(xì)胞數(shù)量減少以及 ED-A+ 纖連蛋白沉積和 α-平滑肌肌動蛋白陽性細(xì)胞數(shù)量得到證實(shí)[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (240-270 g)[4]
Dosage: 12 mg/kg
Administration: Intraperitoneal injection; daily; for 14 or 21 days
Result: Attenuated interstitial fibrosis in rat kidney after unilateral obstruction.
分子量

234.30

Formula

C16H14N2

CAS 號
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 50 mg/mL (213.40 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 4.2680 mL 21.3402 mL 42.6803 mL
5 mM 0.8536 mL 4.2680 mL 8.5361 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.90%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.2680 mL 21.3402 mL 42.6803 mL 106.7008 mL
5 mM 0.8536 mL 4.2680 mL 8.5361 mL 21.3402 mL
10 mM 0.4268 mL 2.1340 mL 4.2680 mL 10.6701 mL
15 mM 0.2845 mL 1.4227 mL 2.8454 mL 7.1134 mL
20 mM 0.2134 mL 1.0670 mL 2.1340 mL 5.3350 mL
25 mM 0.1707 mL 0.8536 mL 1.7072 mL 4.2680 mL
30 mM 0.1423 mL 0.7113 mL 1.4227 mL 3.5567 mL
40 mM 0.1067 mL 0.5335 mL 1.0670 mL 2.6675 mL
50 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1340 mL
60 mM 0.0711 mL 0.3557 mL 0.7113 mL 1.7783 mL
80 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL
100 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

產(chǎn)品名稱:
AG 1295
目錄號:
HY-101957
需求量: