CD437 (DC10491) chemical structure
Chemical structureResearch use only
CAT. NO. DC10491Featured

CD437

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Product overview

Description & Application

CD437 is a retinoid-like research compound with direct DNA polymerase α inhibition and antiproliferative activity in cancer-cell models.

ParameterValue
Chemical Name2-Naphthalenecarboxylicacid, 6-(4-hydroxy-3-tricyclo[3.3.1.13,7]dec-1-ylphenyl)-
CAS No.125316-60-1
Synonyms2-Naphthalenecarboxylicacid, 6-(4-hydroxy-3-tricyclo[3.3.1.13,7]dec-1-ylphenyl)-; O-Desmethyl Adapalene; CD 437; 6-[3-(1-Adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid AHPN; AHPN; ADAP-IME; 6-[3-(1-Adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid; Adapalene IMpurity F; AHPN, 6-[3-(1-Adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid; 6-(4-hydroxy-3-tricyclo(3.3.1.1(3,7))dec-1-ylphenyl)-2-naphthalenecarboxylic; 2-naphthalenecarboxylicacid,6-(4-hydroxy-3-tricyclo(3.3.1.1(3,7))dec-1-ylphen; Apoptosis Activator VI, CD437; 6-[3-(1-Adamantyl)-4-hydroxyphenyl]-2-naphthalenecarboxylic acid; CD 437/AHPN; Apoptosis Activator VI, CD437/AHPN; CD437
FormulaC27H26O3
M.Wt398.49354
SMILESO=C(C1=CC=C2C=C(C3=CC=C(O)C(C4(C5)CC6CC5CC(C6)C4)=C3)C=CC2=C1)O
PurityOn request
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
DNA polymerase α / POLA1 · Literature evidence

Biological Activity

CD437 is a retinoid-like research compound with direct DNA polymerase α inhibition and antiproliferative activity in cancer-cell models. Wild-type POLA1 IC50: 22 nM. Resistant L700S and L764S variants gave IC50 values of 1.2 and 2.6 µM.

In Vitro

EndpointModel / conditions / sourceReported result
POLA1 inhibitionRecombinant DNA polymerase-α activity assay. [1], Fig. 3Wild-type POLA1 IC50: 22 nM. Resistant L700S and L764S variants gave IC50 values of 1.2 and 2.6 µM.
Direct bindingPOLA1 binding measurement. [1], Fig. 4Kd was 67 ± 22 nM. This binding affinity is distinct from the enzymatic IC50.
DNA replicationHCT116 cells; CD437 1.5 µM for 2 h; BrdU incorporation. [1]DNA synthesis was inhibited. Resistant clones required at least 15 µM for comparable inhibition.
Cell-death mechanismSensitive versus POLA1-mutant cells. [1]S-phase effects and caspase-3-associated apoptosis supported a link between POLA1 inhibition and cytotoxicity.

In Vivo

No compound-specific animal efficacy result is established by the sources summarized here.

Interpretation

Its anticancer mechanism should not be described solely as retinoic-acid-receptor agonism.

Original studies

References

  1. Han T, et al. The antitumor toxin CD437 is a direct inhibitor of DNA polymerase α. Nature chemical biology (2016).

Product documentation

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

For additional quantities or product documentation, contact info@dcchemicals.com.

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