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  2. TGF-beta/Smad
  3. TGF-β Receptor
  4. AZ12799734

AZ12799734 是一種選擇性的、具有口服活性的 TGFBR1 激酶抑制劑， IC50 為 47 nM。 AZ12799734 也是一種 BMP 和 TGFβ 抑制劑。

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AZ12799734 Chemical Structure

AZ12799734 Chemical Structure

CAS No. : 1117684-36-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1141
In-stock
1 mg ￥604
In-stock
5 mg ￥1400
In-stock
10 mg ￥2250
In-stock
25 mg ￥4938
In-stock
50 mg 現(xiàn)貨 詢價(jià)
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

查看 TGF-β Receptor 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

AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor[1].

IC50 & Target

TGFBR1

47 nM (IC50)

ALK6

0.017 μM (Kd)

ALK5

0.74 μM (Kd)

ALK4

1 μM (Kd)

ACVR1

6.2 μM (Kd)

ALK1

7.1 μM (Kd)

BMPR1A

40 μM (Kd)

BMP

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDA-MB-468 IC50
22 nM
Compound: 19
Inhibition of ALK5 in human MDA-MB-468 cells assessed as inhibition of nuclear translocation of GFP-2/Smad2 fusion reporter gene after 90 mins by Hoechst 3342 staining-based cellomics arrayscan imaging analysis
Inhibition of ALK5 in human MDA-MB-468 cells assessed as inhibition of nuclear translocation of GFP-2/Smad2 fusion reporter gene after 90 mins by Hoechst 3342 staining-based cellomics arrayscan imaging analysis
[PMID: 19736928]
Sf21 IC50
72 nM
Compound: 19
Inhibition of 6His-tagged human ALK5 expressed in baculovirus-infected SF21 cells after 30 mins by fluorescence polarization assay
Inhibition of 6His-tagged human ALK5 expressed in baculovirus-infected SF21 cells after 30 mins by fluorescence polarization assay
[PMID: 19736928]
體外研究
(In Vitro)

AZ12799734 inhibits ligand activated SMAD3/4 transcription[1].
AZ12799734 (10 nM; 24 h) inhibits phosphorylation of both SMAD1 and SMAD2[1].
AZ12799734 (500 nM; 36 h) inhibits TGFβ-induced migration in HaCaT epithelial cells[1].

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

Western Blot Analysis[1]

Cell Line: HaCaT cells and NIH3T3 cells
Concentration: 10 nM
Incubation Time: 10 days (HaCaT) or 24 h (NIH3T3)
Result: Blocked TGFβ-mediated induction of SMAD2 phosphorylation. Inhibited phosphorylation of both SMAD1 and SMAD2.

Cell Migration Assay [1]

Cell Line: HaCaT epithelial cells
Concentration: 500 nM
Incubation Time: 36 h
Result: A dose-dependent decrease in TGFβ-induced migration was observed.
體內(nèi)研究
(In Vivo)

AZ12799734 (0-400 mg/kg/day; p.o.; 3-7 days) induces histopathologic heart valve lesions in rat[2].
AZ12799734 (50 mg/kg; p.o.; once) shows total and free pharmacokinetic (PK) levels in the nude mouse with time over in vitro IC50 of 0.01885 μM[1].

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

Animal Model: Ten-week-old female HsdHan:WIST rats[2]
Dosage: 200 and 400 mg/kg/day
Administration: Oral, 3-7 days
Result: Hemorrhage into the heart valves was evident at low magnification and the normal architecture of the leaflet was replaced by hemorrhage.
Increased valvular interstitial cells in size and number and shows increased cytoplasm, an enlarged round to spindeloid nucleus, and frequently undergoing mitosis.
Animal Model: Female BALB/c mice[1]
Dosage: 50 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Showed total and free pharmacokinetic (PK) levels with time over in vitro IC50 of 0.01885 μM.
分子量

370.43

Formula

C18H18N4O3S
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 125 mg/mL (337.45 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(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6996 mL 13.4978 mL 26.9957 mL
5 mM 0.5399 mL 2.6996 mL 5.3991 mL
查看完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(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(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)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
參考文獻(xiàn)

AZ12799734 相關(guān)分類

完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(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 2.6996 mL 13.4978 mL 26.9957 mL 67.4891 mL
5 mM 0.5399 mL 2.6996 mL 5.3991 mL 13.4978 mL
10 mM 0.2700 mL 1.3498 mL 2.6996 mL 6.7489 mL
15 mM 0.1800 mL 0.8999 mL 1.7997 mL 4.4993 mL
20 mM 0.1350 mL 0.6749 mL 1.3498 mL 3.3745 mL
25 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6996 mL
30 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2496 mL
40 mM 0.0675 mL 0.3374 mL 0.6749 mL 1.6872 mL
50 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
60 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
80 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8436 mL
100 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 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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產(chǎn)品名稱：
AZ12799734
目錄號(hào)：
HY-123900
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