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Medchemexpress LLC Lerociclib dihydrochloride | 2097938-59-3 | 98.5% | 547.52 | 100 MG
SDP

Catalog No. 5000438358
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Lerociclib dihydrochloride is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM for CDK4/CyclinD1 and 2 nM for CDK6/CyclinD3. It induces a robust and sustained G1 arrest in CDK4/6 dependent cells (EC50 of approximately 20 nM) and complete inhibition of RB phosphorylation. This compound inhibits proliferation in various tumor cell lines, including breast, melanoma, leukemia, and lymphoma. It has demonstrated tumor regression in HER2+ breast cancer models and significant tumor growth inhibition in MCF7 and ER+ ZR-75-1 xenograft models. Clinical trials are underway for advanced breast cancer, endometrial carcinoma, and non-small-cell lung carcinoma.

  • Potent and selective CDK4/CDK6 inhibitor
  • Induces G1 arrest in CDK4/6 dependent cells
  • Inhibits RB phosphorylation
  • Reduces proliferation in various tumor cell lines
  • Demonstrates tumor regression in HER2+ breast cancer models

Catalog No. 50-004-38358 Supplier Medchemexpress LLC Supplier No. HY112272A100MG
May include imposed supplier surcharges.
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Lerociclib dihydrochloride is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM for CDK4/CyclinD1 and 2 nM for CDK6/CyclinD3. It induces a robust and sustained G1 arrest in CDK4/6 dependent cells (EC50 of approximately 20 nM) and complete inhibition of RB phosphorylation. This compound inhibits proliferation in various tumor cell lines, including breast, melanoma, leukemia, and lymphoma. It has demonstrated tumor regression in HER2+ breast cancer models and significant tumor growth inhibition in MCF7 and ER+ ZR-75-1 xenograft models. Clinical trials are underway for advanced breast cancer, endometrial carcinoma, and non-small-cell lung carcinoma.

  • Potent and selective CDK4/CDK6 inhibitor
  • Induces G1 arrest in CDK4/6 dependent cells
  • Inhibits RB phosphorylation
  • Reduces proliferation in various tumor cell lines
  • Demonstrates tumor regression in HER2+ breast cancer models

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