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Numidargistat dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Numidargistat dihydrochloride图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
CB-1158 dihydrochloride
INCB01158 dihydrochloride
产品介绍
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。
生物活性

Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor ofarginase, withIC50s of 86 nM and 296 nM forrecombinant humanarginase1andrecombinant humanarginase2, 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 is a potent and orally-bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC50s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC50, 122 nM). Numidargistat dihydrochloride also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC50s of 32, 139, 210 μM, respectively. Numidargistat dihydrochloride shows no effect on NOS. In addition, Numidargistat dihydrochloride is not directly cytotoxic to murine cancer cell lines[1].

体内研究
(In Vivo)

Numidargistat dihydrochloride (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat dihydrochloride in combination with PD-L1 blockade or LY 188011 inhibits tumor growth in mice bearing CT26 cancer cells[1].

分子量

360.04

性状

Solid

Formula

C11H24BCl2N3O5

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
In Vitro: 

DMSO : 55 mg/mL(152.76 mM;Need ultrasonic)

H2O : 37.78 mg/mL(104.93 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7775 mL13.8873 mL27.7747 mL
5 mM0.5555 mL2.7775 mL5.5549 mL
10 mM0.2777 mL1.3887 mL2.7775 mL
*

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℃, 6 months; -20℃, 1 month (stored under nitrogen, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (277.75 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 3.25 mg/mL (9.03 mM); Suspended solution; Need ultrasonic

    此方案可获得 3.25 mg/mL (9.03 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    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); Clear solution

  • 4.

    请依序添加每种溶剂: 5% DMSO    95% (20%SBE-β-CDin saline)

    Solubility: ≥ 1.38 mg/mL (3.83 mM); Clear solution

*以上所有助溶剂都可在本网站选购。