2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis
  3. Lactate Dehydrogenase Reactive Oxygen Species (ROS) Apoptosis
  4. NCI-006

NCI-006 是一种具有口服活性的乳酸脱氢酶 (LDH) 抑制剂 (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM)。NCI-006 在小鼠胰腺癌模型中抑制了肿瘤内 LDH 活性、乳酸生成、肿瘤生长。NCI-006 在体外抑制糖酵解，诱导细胞凋亡 (apoptosis)。NCI-006 与电离辐射 (IR) 结合使用可以增强糖酵解肿瘤细胞系的放射敏感性，同时不影响非糖酵解/正常细胞 (1522，皮肤成纤维细胞)。NCI-006 与 IACS-010759 (HY-112037) 联合使用对结直肠癌和胃癌发挥协同抗肿瘤作用。NCI-006 通过抑制乳酸脱氢酶靶向糖酵解会损害尤文肉瘤模型中的肿瘤生长。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

NCI-006

NCI-006 Chemical Structure

CAS No. : 1964516-64-0

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

NCI-006 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targeting glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model[1][2][3][4][5][6][7].

体外研究
(In Vitro)

NCI-006 (0-1 μM) 可抑制人乳酸脱氢酶 (hLDH) 以及 HEK293T 细胞乳酸脱氢酶同工酶 2、3、4、5 和小鼠同工酶 1、2、3、4、5 的活性，但不抑制从人肾中分离的苹果酸脱氢酶 (MDH) 和琥珀酸脱氢酶 (SDH) 的活性[3]。
NCI-006 (0.2-5 μM，2 小时) 可降低 MIA PaCa-2 和 HT29 细胞中的 NAD/NADH 比率，影响小鼠 (m) 和人类 (h) 红细胞 (RBC) 以及 MIA PaCa-2 和 HT29 细胞中的乳酸分泌，EC50s 分别为 1.6、2.1、0.37、0.53 μM[3]。
NCI-006 (0-10 μM，0-180 分钟) 在最低浓度为 1 μM 时以时间依赖性方式降低基础细胞外酸化速率 (ECAR)，并在浓度 ≥ 1 μM 时抑制糖酵解，并提高 MIA PaCa-2 细胞中的基础耗氧率 (OCR)[3]。
NCI-006 (1 μM) 与 IACS-010759 (HY-112037) 联合使用可降低 MIA PaCa-2、HCT116 和 MKN45细胞的细胞活力[3][6]。
NCI-006 (5 μM) 在 HCT116 和 MKN45 细胞中可降低 OCR、ECAR 和糖 ATP 生成速率，但不影响线粒体 ATP 生成速率或总 ATP 生成速率，也不会增加有丝分裂期 ATP 生成速率，但与 IACS-010759 (HY-112037) 联合使用可显著增加糖 ATP 生成速率[6]。
NCI-006 (72 小时) 抑制尤文肉瘤细胞系增殖，IC50s 范围为 100 nmol/L (TC71 和 TC32) 至 1 μmol/L (RDES 和 EW8)，对横纹肌肉瘤和骨肉瘤无作用，IC50 为 1,037 nmol/L[7]。
NCI-006 剂量依赖性地抑制 TC71、TC32、EW8 细胞中的 LDH 活性，IC50 约为100 nmol/L[7]。
NCI-006 (0.1-10 μM，2 小时) 可抑制 TC71 和 EW8 细胞中的ECAR[7]。

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

NCI-006 相关抗体:
体内研究
(In Vivo)

NCI-006 (0-200 mg/kg，口服/静脉注射，一次) 在 2 小时内可降低雌性无胸腺裸鼠的 LDH 活性[3]。
NCI-006 (50 mg/kg，口服/静脉注射，一次；静脉注射，隔日一次，持续 1 周或 2 周) 在 MIA PaCa-2/HT29肿瘤雌性无胸腺裸鼠中可抑制肿瘤 LDH 活性，导致丙酮酸转化为乳酸的转化率降低，丙酮酸向碳酸氢盐的通量和线粒体氧化作用增强，同时转氨酶介导的丙酮酸向丙氨酸的通量未见明显增加，从而减缓了肿瘤生长[3]。
NCI-006 (40 mg/kg，静脉注射，每周 2/3 次，持续 1/2 周) 单独治疗不能抑制肿瘤生长，与 IACS-010759 (HY-112037) 联合使用可抑制 HCT116 和 MKN45 异种移植裸鼠中的肿瘤生长[6]。
NCI-006 (50 mg/kg，口服，每日一次或两次，3 周) 对 TC71、TC32 和 EW8 异种移植雌性 Fox Chase SCID 米色小鼠中的肿瘤生长几乎没有影响[7]。

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

Animal Model: Female athymic nude mice (20-25 g)[3]
Dosage: 0 mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: p.o., once
Result: Dose-dependent reduced LDH activity at 2 h, but in most cases, recovery to baseline levels by 24 h, 75%-80% of baseline at 24 h, with maximal inhibition maintained at 8 h.
Animal Model: Female athymic nude mice (20-25 g)[3]
Dosage: 0 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: i.v., once
Result: Dose-dependent reduced LDH activity at 2 h, but in most cases, recovery to baseline levels by 24 h.
Animal Model: MIA PaCa-2 tumor female athymic nude mice (20-25 g)[3]
Dosage: 50 mg/kg
Administration: p.o./i.v., once; i.v., every other day for 1 week (three injections, Monday, Wednesday, and Friday), or for 2 weeks (six injections) with a break of 1 week between cycles.
Result: Inhibits LDH by 80% at intratumoral drug levels of approximately 20 μM.
Dose dependently suppressed the tumor [13C]lactate/[13C]pyruvate ratio, did not affect the [13C]lactate/[13C]pyruvate ratio in MIA PaCa-2 tumors (up to 7 h after drug administration).
Slowed the growth of MIA PaCa-2 xenografts without a marked effect on mouse body weight.
Reduced conversion of [13C]pyruvate to both [13C]lactate and [13C]bicarbonate, more significantly inhibits tumor growth in combination with IACS-010759 (HY-112037).
Animal Model: HT29 tumor female athymic nude mice (20-25 g)[3]
Dosage: 50 mg/kg
Administration: i.v., once
Result: Decreased the [13C]Lac/[13C]Pyr ratio by 74.7%.
More significantly inhibits tumor growth when combined with Metformin(HY-B0627).
Animal Model: HCT116 (5×106) xenografts nude mice (18-24 g, six-week-old female KSN/slc athymic)[6]
Dosage: 40 mg/kg
Administration: i.v., 3 times a week, 1 weeks
Result: Treatment alone did not inhibit tumor growth, inhibited tumor growth and transiently and significantly increased AST, ALT, amylase, lipase, creatinine, and bilirubin levels in combination with IACS-010759 (HY-112037).
Decreased the 13C-L/P ratio, increased ROS levels.
Animal Model: MKN45 xenografts nude mice (18-24 g, six-week-old female KSN/slc athymic)[6]
Dosage: 40 mg/kg
Administration: i.v., 2 times a week, 2 weeks
Result: Treatment alone did not inhibit tumor growth, inhibited tumor growth and transiently and significantly increased AST, ALT, amylase, lipase, creatinine, and bilirubin levels in combination with IACS-010759 (HY-112037).
Decreased the 13C-L/P ratio.
Animal Model: TC71, TC32, and EW8 xenografts female Fox Chase SCID beige mice [7]
Dosage: 50 mg/kg
Administration: p.o., once or twice daily, 3 weeks
Result: Had little change in tumor growth.
分子量

650.74

Formula

C31H24F2N4O4S3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NCI-006 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

NCI-0061964516-64-0NCI006NCI 006Lactate DehydrogenaseReactive Oxygen Species (ROS)ApoptosisLDHInhibitorapoptosisglycolysisEwing sarcoma modelMKN45 cellsMIA PaCa-2 cellsHCT116 cellsHT29 cellsnude miceinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
NCI-006
目录号：
HY-176798
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z