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  1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)
  3. Indoximod

Indoximod  (Synonyms: 1-甲基-D-色氨酸; 1-Methyl-D-tryptophan; NLG-8189)

目錄號(hào): HY-16724 純度: 99.04%
COA 產(chǎn)品使用指南

Indoximod (1-Methyl-D-tryptophan) 是一種具有口服活性的吲哚胺2,3-雙加氧酶(IDO) 途徑抑制劑。Indoximod 充當(dāng)Trp模擬物,調(diào)節(jié)mTOR中。Indoximod 是一種可用于癌癥研究的免疫代謝佐劑。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Indoximod Chemical Structure

Indoximod Chemical Structure

CAS No. : 110117-83-4

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Customer Review

Other Forms of Indoximod:

查看 Indoleamine 2,3-Dioxygenase (IDO) 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Indoximod (1-Methyl-D-tryptophan) is an orally active indoleamine 2,3-dioxygenase (IDO) pathway inhibitor. Indoximod acts as a Trp mimetic in regulating mTOR. Indoximod is an immunometabolic adjuvant used for the research of cancer[1][2].

IC50 & Target[1]

IDO

19 μM (Ki)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: D-MT
Anticancer activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 31954880]
HeLa IC50
> 100 μM
Compound: D-MT
Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 31954880]
HeLa EC50
110 μM
Compound: L-1MT
Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate after 24 hrs
Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate after 24 hrs
[PMID: 28526475]
HUVEC IC50
> 100 μM
Compound: D-MT
Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 31954880]
PC-3 IC50
> 100 μM
Compound: D-MT
Anticancer activity against human PC3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Anticancer activity against human PC3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 31954880]
U-87MG ATCC IC50
148.9 μM
Compound: 1-D-MT
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
[PMID: 27475108]
體外研究
(In Vitro)

The IDO inhibitor 1-methyl-tryptophan exists in two stereoisomers with potentially different biological properties. The L isomer is the more potent inhibitor of IDO activity using the purified enzyme and in HeLa cell–based assays. However, the D isomer is significantly more effective in reversing the suppression of T cells created by IDO-expressing dendritic cells. The L isomer of 1-methyl-tryptophan functioned as a competitive inhibitor (Ki=19 μM), whereas the d isomer is much less effective. The DL mixture is intermediate, with a Ki of 35 μM[1].

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

體內(nèi)研究
(In Vivo)

The D isomer is more efficacious as an anticancer agent in chemo-immunotherapy regimens using NSC-26271, NSC 125973, or LY 188011, when tested in mouse models of transplantable melanoma and transplantable and autochthonous breast cancer. The D isomer of 1-methyl-tryptophan specifically targets the IDO gene because the antitumor effect of d-1-methyl-tryptophan is completely lost in mice with a disruption of the IDO gene (IDO-knockout mice). Oral administration of dl-1-methyl-tryptophan in combination with NSC 125973 can elicit regression of autochthonous breast tumors[1].

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

Clinical Trial
分子量

218.25

Formula

C12H14N2O2

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

1-甲基-D-色氨酸

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): 

H2O 中的溶解度 : 5 mg/mL (22.91 mM; 超聲助溶; 酸性條件溶解 (HCL 調(diào)節(jié),pH≈2))

DMSO 中的溶解度 : 0.55 mg/mL (2.52 mM; 超聲加熱助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)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 4.5819 mL 22.9095 mL 45.8190 mL
5 mM 0.9164 mL 4.5819 mL 9.1638 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。

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

  • 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):

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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: PBS

    Solubility: 1 mg/mL (4.58 mM); 澄清溶液; 超聲助溶 (<60°C)

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

由于實(shí)驗(yàn)過(guò)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
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,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.85%

參考文獻(xiàn)
Kinase Assay
[1]

1MT enantiomers are solubilized in DMSO containing 0.1N HCl and added at concentrations of 100, 50, and 0 μM to wells containing the reaction mixture with tryptophan (0-200 μM) followed by addition of IDO enzyme. Plates are sealed and incubated 1 hr in a humidified 37°C incubator, after which the reactions are terminated by addition of 12.5 μl 30% TCA per well. Plates are then resealed in plastic wrap, incubated 30 min at 50°C to hydrolyze the reaction product N-formylkynurenine to kynurenine, and centrifuged. Supernatants are transferred to a flat-bottom 96-well plate, mixed with 100 μl Ehrlich reagent and incubated 10 min at room temperature. Absorbance at 490 nm is read[1].

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

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 / H2O 1 mM 4.5819 mL 22.9095 mL 45.8190 mL 114.5475 mL
H2O 5 mM 0.9164 mL 4.5819 mL 9.1638 mL 22.9095 mL
10 mM 0.4582 mL 2.2910 mL 4.5819 mL 11.4548 mL
15 mM 0.3055 mL 1.5273 mL 3.0546 mL 7.6365 mL
20 mM 0.2291 mL 1.1455 mL 2.2910 mL 5.7274 mL

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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:
Indoximod
目錄號(hào):
HY-16724
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