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  2. TGF-beta/Smad
  3. TGF-β Receptor
  4. LDN-214117

LDN-214117 是一種 ALK2 抑制劑，具有口服活性，耐受性好，腦穿透性好。LDN-214117 對(duì) ALK2 具有較高的選擇性和較低的細(xì)胞毒性，其 IC50 值為 24 nM。LDN-214117 也是一種特異性的骨形態(tài)發(fā)生蛋白 (BMPs) 信號(hào)抑制劑，對(duì) BMP6 具有相對(duì)選擇的抑制作用，其 IC50 值為 100 nM。LDN-214117 可用于進(jìn)行性骨化性纖維發(fā)育不良 (FOP) 和彌漫性內(nèi)源性橋腦膠質(zhì)瘤 (DIPG) 的研究。

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LDN-214117 Chemical Structure

LDN-214117 Chemical Structure

CAS No. : 1627503-67-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥600
In-stock
10 mg ￥1100
In-stock
25 mg ￥2200
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50 mg ￥3800
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100 mg ￥5900
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

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

LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [1][2]

IC50 & Target

IC50: 24 nM (ALK2); 27 nM (ALK1); 1,171 nM (ALK3); 3,000 nM (ALK5); 1,022 nM (BMP6); 27 nM (BMP2); 960 nM (BMP4); 16,000 nM (TGF-β1)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
C2C12 IC50
100 nM
Compound: 10, LDN-214117
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
C2C12 IC50
1022 nM
Compound: 10, LDN-214117
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
C2C12 IC50
960 nM
Compound: 10, LDN-214117
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
1171 nM
Compound: 10, LDN-214117
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
16000 nM
Compound: 10, LDN-214117
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
27 nM
Compound: 10, LDN-214117
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
27 nM
Compound: 10, LDN-214117
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
體外研究
(In Vitro)

LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50 value of 24 nM[1].
LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50 values of 27 nM, 1,171 nM and 3,000 nM, respectively[1].
LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50 values of 100 nM, 1,022 nM and 960 nM, respectively[1].
LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50 values of 16,000 nM[1].
LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting[2].
LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H[2].
LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells[2].
LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids[2].

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

Cell Viability Assay[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h, 72 h and 96 h
Result: Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point.

Western Blot Analysis[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 30 min, 3 h and 24 h
Result: Diminished the increase of ID1 protein.

Apoptosis Analysis[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h, 72 h and 96 h
Result: Induced considerable death of LCLC-103H cells.

RT-PCR[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h and 72 h
Result: Induced distinct gene expression patterns for the two EMTTFs.

Cell Migration Assay [2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 0 h, 24 h and 48 h
Result: Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.
體內(nèi)研究
(In Vivo)

LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice[3].

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

Animal Model: NOD.SCID mice[3]
Dosage: 25 mg/kg
Administration: p.o., daily, for 14 days
Result: Showed good-tolerated in mice.
分子量

419.52

Formula

C25H29N3O3
CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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 : 20 mg/mL (47.67 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)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 2.3837 mL 11.9184 mL 23.8368 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(qǐng)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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?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(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.77 mM); 澄清溶液

    此方案可獲得 ≥ 2 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.77 mM); 澄清溶液

    此方案可獲得 ≥ 2 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)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(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.92%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(qǐng)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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?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 2.3837 mL 11.9184 mL 23.8368 mL 59.5919 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 mL 11.9184 mL
10 mM 0.2384 mL 1.1918 mL 2.3837 mL 5.9592 mL
15 mM 0.1589 mL 0.7946 mL 1.5891 mL 3.9728 mL
20 mM 0.1192 mL 0.5959 mL 1.1918 mL 2.9796 mL
25 mM 0.0953 mL 0.4767 mL 0.9535 mL 2.3837 mL
30 mM 0.0795 mL 0.3973 mL 0.7946 mL 1.9864 mL
40 mM 0.0596 mL 0.2980 mL 0.5959 mL 1.4898 mL
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產(chǎn)品名稱：
LDN-214117
目錄號(hào)：
HY-16712
需求量：