LEE011 (succinate)

China [CN]

CAS No.: 1374639-75-4

Molecular Formula: C₂₇H₃₆N₈O₅

Molecular Weight: 552.64

Chemical Name: (E)-7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)imino)-3,7-dihydro-2H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate

Appearance: Light beige/pale yellow to brown powder

Melting Point: >160°C (decomposes)

Solubility: Slightly soluble in DMSO and methanol; almost insoluble in water

Storage: -20°C frozen / 2–8°C refrigerated, sealed, dry, and protected from light

Purity: ≥98%, ≥99% (mainstream for export)

II. Core Mechanism of Action (Scientific Research/ (Pharmaceutical Selling Points)

Target: Highly selective inhibition of CDK4/6 (cyclin-dependent kinases 4/6)

IC₅₀: CDK4 = 10 nM; CDK6 = 39 nM; 1000-fold lower inhibitory activity against CDK1

Mechanism: Blocks Rb protein phosphorylation, arresting tumor cells in the G0/G1 phase and inhibiting proliferation

Oral bioavailability: Good, used for preclinical/clinical research in solid tumors

III. Main Applications (Pharmaceuticals/Research)

Anti-tumor: Model studies of breast cancer (HR+/HER2-), melanoma, lung cancer, neuroblastoma, etc.

Combination therapy: Enhanced anti-tumor effects when used in combination with endocrine drugs, PI3K inhibitors, and BRAF inhibitors.

Purpose: For research experiments only; not for direct human treatment.

IV. Key Indicators for Foreign Trade/Quality Inspection (COA) (Commonly Used)

Content: 98.0%–102.0%

Single Impurity: ≤0.1%; Total Impurities: ≤1.0%

Loss on Drying: ≤0.3%; Residue on Ignition: ≤0.1%

Heavy Metals: ≤20 ppm; Succinic Acid Content: 20.8%–21.9%

Packaging: 100mg/bottle, 1g/bottle, 1kg/aluminum foil bag/fluorinated bottle