565434-85-7
Chemical Structure
CBP-501
- CAS No.: 565434-85-7
- Formula:C86H122F5N29O17
- Molecular Weight:1929.06
IUPAC Name: ((R)-2-((R)-2-((R)-2-((R)-2-((R)-2-((R)-2-amino-3-(4-benzoylphenyl)propanamido)-3-hydroxypropanamido)-3-(1H-indol-3-yl)propanamido)-3-hydroxypropanamido)-3-(perfluorophenyl)propanamido)-3-cyclohexylpropanoyl)-D-arginyl-D-arginyl-D-arginyl-D-glutaminyl-D-arginyl-D-arginine
InChIKey: DEZJGRPRBZSAKI-KMGSDFBDSA-N
SMILES: N=C(N)NCCC[C@H](C(O)=O)NC([C@@H](CCCNC(N)=N)NC([C@@H](CCC(N)=O)NC([C@@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)NC([C@@H](CCCNC(N)=N)NC([C@@H](CC1CCCCC1)NC([C@@H](CC2=C(F)C(F)=C(F)C(F)=C2F)NC([C@@H](CO)NC([C@@H](CC3=CNC4=CC=CC=C34)NC([C@@H](CO)NC([C@@H](CC5=CC=C(C(C6=CC=CC=C6)=O)C=C5)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer[1][2].
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CBP-501 | CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer. | |||||||||||||||||||||
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References
- [1]. Enzler T, et al. A multicenter, randomized phase 2 study to establish combinations of CBP501, cisplatin and nivolumab for ≥3rd-line treatment of patients with advanced pancreatic adenocarcinoma. Eur J Cancer. 2024 Apr;201:113950. [Content Brief]
- [2]. Shi-Ken Sha, et al. Cell cycle phenotype-based optimization of G2-abrogating peptides yields CBP501 with a unique mechanism of action at the G2 checkpoint. Mol Cancer Ther. 2007 Jan;6(1):147-53. [Content Brief]
