1. Metabolic Enzyme/Protease
  2. Aldehyde Dehydrogenase (ALDH)
  3. CLM296

CLM296 是一种强效且选择性的 ALDH1A3 抑制剂,其 IC50 为 2 nM。CLM296 对高度同源的 ALDH1A1 异构体没有脱靶效应。CLM296 可抑制 ALDH1A3 驱动的乳腺癌肿瘤转移。CLM296 可用于研究三阴性乳腺癌 (TNBC)。

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CLM296 Chemical Structure

CLM296 Chemical Structure

CAS No. : 3067837-25-3

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查看 Aldehyde Dehydrogenase (ALDH) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CLM296 is a potent and selective ALDH1A3 inhibitor with an IC50 of 2 nM. CLM296 has no off-target effects on the highly homologous ALDH1A1 isoform. CLM296 inhibits ALDH1A3-driven tumor metastasis in breast cancer. CLM296 can be used for the study of triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

ALDH1A3

2 nM (IC50)

体外研究
(In Vitro)

CLM296 (0.01 nM-10 μM) 显著降低 ALDH1A3 过表达的 MDA-MB-231 细胞、MDA-MB-468 和 HCC1806 shRNA 对照细胞中的 AldefluorTM 荧光,IC50 值分别为 2.1 nM、2.5 nM 和 2.3 nM[1]
CLM296 (1 μM;72 小时) 不影响 MDA-MB-231、MDA-MB-468 或 HCC1806 细胞中的细胞死亡或增殖[1]
CLM296 (100 nM;24 小时) 特异性降低 ALDH1A3 过表达对 MDA-MB-231 细胞侵袭性的增强[1]
CLM296 (1-100 nM;24 小时) 可特异性阻断 MDA-MB-231 细胞中 ALDH1A3 介导的基因表达变化[1]

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

Cell Viability Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 and HCC1806 cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Results: Did not affect cell death or proliferation in MDA-MB-231, MDA-MB-468 or HCC1806 cells.

Cell Invasion Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Specifically reduced the increased invasion imparted by ALDH1A3 overexpression in MDA-MB-231 cells.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 1 nM , 10 nM , 100 nM
Incubation Time: 24 h
Result: Significantly reduced expression of ALDH1A3-induced genes, RARβ, ELF3, and DHRS3.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Mice 4 mg/kg i.p. Tmax 1 hr
Mice 4 mg/kg p.o. Cmax 10.97 μM
Mice 4 mg/kg i.p. Cmax 24.24 μM
Mice 4 mg/kg p.o. Tmax 4 hr
Mice 4 mg/kg i.p. AUC0-∞ 233.4 μM/L·h
Mice 4 mg/kg p.o. AUC0-∞ 128.5 μM/L·h
Mice 4 mg/kg i.p. T1/2 (Elimination) 8.62 hr
Mice 4 mg/kg p.o. T1/2 (Elimination) 12.9 hr
Mice 4 mg/kg i.p. CLapparent 39.8 mL/h/kg
Mice 4 mg/kg p.o. CL 72.2 mL/h/kg
Mice 4 mg/kg i.p. Vd 494400 L/kg
Mice 4 mg/kg p.o. Vd 1.35 L/kg
体内研究
(In Vivo)

CLM296 (0-4 mg/kg;腹膜内 (IP) 注射;每日一次;连续 42 天;细胞注射后 12 或 15 天) 显著降低了 ALDH1A3 过表达肿瘤小鼠的肿瘤体积和转移[1]

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

Animal Model: Female non-obese diabetic severe combined immunodeficient (NOD-SCID) mice (6-12 weeks old) were orthotopically implanted with MDA-MB-231 cells ( 2x106)[1].
Dosage: 0 mg/kg, 0.4 mg/kg, or 4 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; for 42 days; 15 days after cell injection
Result: Significantly reduced tumor volumes in only the mice bearing tumors with ALDH1A3 overexpression.
Animal Model: Female non-obese diabetic severe combined immunodeficient (NOD-SCID) mice (6-12 weeks old) were orthotopically implanted with MDA-MB-231 cells ( 2x106)[1].
Dosage: 0 mg/kg, 0.4 mg/kg, or 4 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; for 42 days; 12 days after cell injection
Result: Reduced metastasis in the MDA622 MB-231 model with ALDH1A3 overexpression.
分子量

430.50

Formula

C29H22N2O2

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
  • 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.

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产品名称:
CLM296
目录号:
HY-174209
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