1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. Arginase
  3. Numidargistat dihydrochloride

Numidargistat dihydrochloride  (Synonyms: CB-1158 dihydrochloride; INCB01158 dihydrochloride)

目录号: HY-101979A 纯度: 98.65%
COA 产品使用指南

Numidargistat (CB-1158) dihydrochloride 是一种有效的,具有口服活性的精氨酸酶 (arginase) 抑制剂,对重组人 arginase 1arginase 2IC50 值分别为 86 nM 和 296 nM。免疫肿瘤剂。

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Numidargistat dihydrochloride Chemical Structure

Numidargistat dihydrochloride Chemical Structure

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2750
In-stock
5 mg ¥2500
In-stock
10 mg ¥4500
In-stock
25 mg ¥9500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Numidargistat dihydrochloride:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor of arginase, with IC50s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent[1].

IC50 & Target

IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)[1]

体外研究
(In Vitro)

Numidargistat dihydrochloride 是一种有效的口服生物利用度精氨酸酶抑制剂,对重组人精氨酸酶 1 和 2 的 IC50 分别为 86 和 296 nM。Numidargistat dihydrochloride 抑制人粒细胞、红细胞和肝细胞裂解物中的天然精氨酸酶 1 (Arg1),IC50 分别为 178 nM、116 nM 和 158 nM,并阻断癌症患者血浆中的 Arg1 (IC 50,122 nM)。Numidargistat dihydrochloride 还对人 HepG2、K562 细胞系和原代人肝细胞中的精氨酸酶表现出有效的抑制活性,IC50 分别为 32、139、210 μM。Numidargistat dihydrochloride 对 NOS 没有影响。此外,Numidargistat dihydrochloride 对小鼠癌细胞系没有直接的细胞毒性[1]

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

体内研究
(In Vivo)

Numidargistat dihydrochloride (100 mg/kg,口服,每天两次) 增加小鼠肿瘤浸润细胞毒性细胞的数量并减少骨髓细胞。Numidargistat dihydrochloride 与 PD-L1 阻断剂或 LY 188011 联合抑制携带 CT26 癌细胞的小鼠的肿瘤生长[1]

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

分子量

360.04

Formula

C11H24BCl2N3O5

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 55 mg/mL (152.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 37.78 mg/mL (104.93 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7775 mL 13.8873 mL 27.7747 mL
5 mM 0.5555 mL 2.7775 mL 5.5549 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 3.25 mg/mL (9.03 mM); 悬浊液; 超声助溶

    此方案可获得 3.25 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.75 mg/mL (7.64 mM); 澄清溶液

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (277.75 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 98.65%

参考文献
Cell Assay
[1]

Intracellular arginase activity is determined for the arginase-expressing HepG2 and K-562 cell lines as follows. HepG2 cells are seeded at 100,000 cells per well one day prior to treatment with CB-1158. K-562 cells are seeded at 200,000 cells per well on the day of CB-1158 treatment. Cells are treated with a dose-titration of CB-1158 in SILAC RPMI-1640 media containing 5% heat-inactivated and dialyzed FBS, antibiotics/anti-mycotic, 10 mM L-arginine, 0.27 mM L-lysine, and 2 mM L-glutamine. The medium is harvested after 24 h and urea generated is determined. Wells containing media without cells are used as background controls. For assessing the effect of CB-1158 on Arg1 in primary hepatocytes, frozen human hepatocytes are thawed, allowed to adhere onto collagen-coated wells for 4 h, and then incubated for 48 h in SILAC-RPMI containing 10 mM L-ornithine, no L-arginine, and a dose-titration of CB-1158, at which time the media are analyzed for urea[1].

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

Animal Administration
[1]

Mice[1]
For the 4T1 tumor model, 105 cells are injected orthotopically into the mammary fat pad; for all other tumor models, 106 cells are injected subcutaneously (s.c.) in the right flank. For all studies, CB-1158 is administered by oral gavage twice per day at 100 mg/kg starting on study day 1 (1 day after tumor implant). Control groups receive vehicle (water) twice daily by gavage. Tumor volume measured by digital caliper (length × width × width/2) and body weight are recorded three times per week. Mice are euthanized when tumors necrotize or volumes reach 2000 mm3. For the CT26 model, anti-PD-L1 antibody (5 mg/kg) is injected intraperitoneally (i.p.) on days 5, 7, 9, 11, 13, and 15. For the 4T1 model, anti-CTLA-4 antibody (5 mg/kg) is injected i.p. on days 2, 5, and 8; anti-PD-1 antibody (5 mg/kg) is injected i.p. on days 3, 6, and 9. 4T1 tumors are harvested on study day 25 into Fekete’s solution and tumor nodules are enumerated visually. LY 188011 is dosed 50 mg/kg i.p. on days 10 and 16 for the CT26 model, 60 mg/kg i.p. on days 6 and 10 for the LLC model, or 30 mg/kg i.p. on day 5 for the 4T1 model. With these regimens, LY 188011 modestly reduces tumor growth and spares most tumor-infiltrating immune cells, allowing for the evaluation of combination activity with CB-1158[1].

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

参考文献

Numidargistat dihydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.7775 mL 13.8873 mL 27.7747 mL 69.4367 mL
5 mM 0.5555 mL 2.7775 mL 5.5549 mL 13.8873 mL
10 mM 0.2777 mL 1.3887 mL 2.7775 mL 6.9437 mL
15 mM 0.1852 mL 0.9258 mL 1.8516 mL 4.6291 mL
20 mM 0.1389 mL 0.6944 mL 1.3887 mL 3.4718 mL
25 mM 0.1111 mL 0.5555 mL 1.1110 mL 2.7775 mL
30 mM 0.0926 mL 0.4629 mL 0.9258 mL 2.3146 mL
40 mM 0.0694 mL 0.3472 mL 0.6944 mL 1.7359 mL
50 mM 0.0555 mL 0.2777 mL 0.5555 mL 1.3887 mL
60 mM 0.0463 mL 0.2315 mL 0.4629 mL 1.1573 mL
80 mM 0.0347 mL 0.1736 mL 0.3472 mL 0.8680 mL
100 mM 0.0278 mL 0.1389 mL 0.2777 mL 0.6944 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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产品名称:
Numidargistat dihydrochloride
目录号:
HY-101979A
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