2387570-00-3
Chemical Structure
DZD1516
- CAS No.: 2387570-00-3
- Formula:C28H27F2N7O3
- Molecular Weight:547.56
InChIKey: IDQNCHCNBVCUHC-DEOSSOPVSA-N
SMILES: COC1=CC2=C(C(NC3=CC=C(C(C)=C3)OC4=CC5=NC=NN5C=C4)=NC=N2)C(O[C@H]6CCN(CC6(F)F)C)=C1
Biological Activity: DZD1516 is an orally active, reversible, blood-brain barrier (BBB)-penetrant selective HER2 tyrosine kinase inhibitor with an IC50 of 0.56 nM against HER2. DZD1516 is not a substrate of P-gp or BCRP, and exhibits high passive permeability. DZD1516 inhibits tumor growth in HER2-positive brain metastasis, leptomeningeal metastasis and subcutaneous xenograft models, and can be used for research related to HER2-positive breast cancer and central nervous system metastasis[1][2][3].
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DZD1516 | 99.62% | DZD1516 is an orally active, reversible, blood-brain barrier (BBB)-penetrant selective HER2 tyrosine kinase inhibitor with an IC50 of 0.56 nM against HER2. DZD1516 is not a substrate of P-gp or BCRP, and exhibits high passive permeability. DZD1516 inhibits tumor growth in HER2-positive brain metastasis, leptomeningeal metastasis and subcutaneous xenograft models, and can be used for research related to HER2-positive breast cancer and central nervous system metastasis. | ||||||||||||||||||||
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References
- [1]. Hu X, et al. Early clinical safety and pharmacokinetics data of DZD1516, an BBB-penetrant selective HER2 inhibitor for the treatment of HER2-positive metastatic breast cancer. Poster Session 1038. 2022.
- [2]. Yang Z, et al. ErbB receptor inhibitors. United States, US20220411422 A1, 2022-12-29.
- [3]. Zhang J, et al. Preclinical and clinical activity of DZD1516, a full blood-brain barrier-penetrant, highly selective HER2 inhibitor. Breast cancer research : BCR. 2023 Jul 06;25(1):81. [Content Brief]
