| Identification | Back Directory | [Name]
Benzonitrile, 4-[2-(4-amino-1-piperidinyl)-5-(3-fluoro-4-methoxyphenyl)-1,6-dihydro-1-methyl-6-oxo-4-pyrimidinyl]-2-fluoro- | [CAS]
1821307-10-1 | [Synonyms]
LSD1-IN-7
Pulrodemstat
Pulrodemstat (CC90011)
Benzonitrile, 4-[2-(4-amino-1-piperidinyl)-5-(3-fluoro-4-methoxyphenyl)-1,6-dihydro-1-methyl-6-oxo-4-pyrimidinyl]-2-fluoro- | [Molecular Formula]
C24H23F2N5O2 | [MOL File]
1821307-10-1.mol | [Molecular Weight]
451.47 |
| Hazard Information | Back Directory | [Uses]
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1]. | [in vivo]
Pulrodemstat (CC-90011; 5 mg/kg; oral administration; daily; for 30 days; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1].
Pulrodemstat (once a day; for 4 days) treatment results in robust downregulation of GRP mRNA levels at 2.5 mg/kg and maximum suppression of GRP at 5 mg/kg in a SCLC human tumor xenograft (H1417) mice[1].
After i.v. administration, Pulrodemstat (Compound 11; 5 mg/kg) has systemic clearance of 32.4 mL/min/kg, elimination half-life of 2 h, and a high volume of distribution of 7.5 L/kg. Pulrodemstat (Compound 11; 5 mg/kg) is readily absorbed after oral administration with an AUC0-24h of 1.8 μM·h, C/sub>max of 0.36 μM, and oral bioavailability of 32%[1]. | Animal Model: | BALB/c nude mice bearing small cell lung carcinoma (SCLC)[1] | | Dosage: | 5 mg/kg | | Administration: | Oral administration; daily; for 30 days | | Result: | Showed a tumor growth inhibition (TGI) of 78% at 5 mg/kg with no body weight loss. |
| [IC 50]
KDM1/LSD1 | [References]
[1] Toufike Kanouni, et al. Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1). J Med Chem. 2020 Dec 10;63(23):14522-14529. DOI:10.1021/acs.jmedchem.0c00978 |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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