CC-90011
CC-90011 Basic information
- Product Name:
- CC-90011
- Synonyms:
-
- CC-90011 besylate
- CC-90011; CC90011; CC 90011; CC-90011 BESYLATE;
- CC-90011
- LSD1-IN-7 benzenesulfonate
- LSD1-IN-7 benzenesulfote
- CC-90011 besylicacid
- CC-90011 benzenesulfonate
- Pulrodemstat benzenesulfonate
- CAS:
- 2097523-60-7
- MF:
- C30H29F2N5O5S
- MW:
- 609.65
- Mol File:
- 2097523-60-7.mol
CC-90011 Chemical Properties
- solubility
- DMSO:62.5(Max Conc. mg/mL);102.52(Max Conc. mM)
- form
- Solid
- color
- Off-white to light yellow
CC-90011 Usage And Synthesis
Uses
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity[1].
in vivo
CC-90011 (5 mg/kg; oral administration; daily; for 30 days) treatment inhibits tumor growth in patient-derived xenograft SCLC models[1].
CC-90011 (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, CC-90011 (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. CC-90011 (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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