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

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).

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CLM296 Chemical Structure

CLM296 Chemical Structure

CAS No. : 3067837-25-3

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Description

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)

In Vitro

CLM296 (0.01 nM-10 μM) significantly reduces AldefluorTM 438 fluorescence in MDA-MB-231 cells with ALDH1A3 overexpression, MDA-MB-468 and HCC1806 shRNA control cells with IC50 values of 2.1 nM, 2.5 nM, and 2.3 nM, respectively[1].
CLM296 (1 μM; 72 h) does not affect cell death or proliferation in MDA-MB-231, MDA-MB-468 or HCC1806 cells[1].
CLM296 (100 nM; 24 h) specifically reduces the increased invasion imparted by ALDH1A3 overexpression in MDA-MB-231 cells [1].
CLM296 (1-100 nM; 24 h) specifically blocks ALDH1A3-mediated gene expression changes in MDA-MB-231 cells [1].

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

CLM296 Related Antibodies

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.
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
In Vivo

CLM296 (0-4 mg/kg; intraperitoneal (IP) injection; once daily; for 42 days; 12 or 15 days after cell injection) significantly reduces tumor volumes and metastasis in the mice bearing tumors with ALDH1A3 overexpression[1].

MedChemExpress (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.
Molecular Weight

430.50

Formula

C29H22N2O2
CAS No.
SMILES

CC(C1=CC=C(C(C=C2C3=CC=C(C(C)=O)C=C3)=CN4C2=NC(C5=CC=CC=C5)=C4)C=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CLM296 Related Classifications

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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:

CLM2963067837-25-3CLM 296CLM-296Aldehyde Dehydrogenase (ALDH)ALDH1A3 inhibitorselectivetriple-negative breast cancer (TNBC)metastasisInhibitorinhibitorinhibit

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