416852-27-2
Chemical Structure
BGC638
- CAS No.: 416852-27-2
- Formula:C32H33N5O9
- Molecular Weight:631.64
IUPAC Name: ((S)-4-carboxy-4-(4-(((S)-2-methyl-4-oxo-4,6,7,8-tetrahydro-1H-cyclopenta[g]quinazolin-6-yl)(prop-2-yn-1-yl)amino)benzamido)butanoyl)-D-glutamic acid
InChIKey: DJBPYPCKXOFYII-USZFVNFHSA-N
SMILES: N(CC#C)([C@@H]1C=2C(=CC3=C(C2)C(=O)N=C(C)N3)CC1)C4=CC=C(C(N[C@@H](CCC(N[C@H](CCC(O)=O)C(O)=O)=O)C(O)=O)=O)C=C4
Biological Activity: BGC638 is a thymidylate synthase inhibitor with a Ki value of 0.24 nM. BGC638 binds to α-FR with high affinity and enters cells via receptor-mediated endocytosis, thereby potently inhibiting thymidylate synthase to block DNA synthesis and ultimately induce apoptosis. BGC638 is applicable to studies related to α-FR-overexpressing tumors and epithelial carcinomas (ovarian cancer and endometrial cancer)[1][2].
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BGC638 | BGC638 is a thymidylate synthase inhibitor with a Ki value of 0.24 nM. BGC638 binds to α-FR with high affinity and enters cells via receptor-mediated endocytosis, thereby potently inhibiting thymidylate synthase to block DNA synthesis and ultimately induce apoptosis. BGC638 is applicable to studies related to α-FR-overexpressing tumors and epithelial carcinomas (ovarian cancer and endometrial cancer). | |||||||||||||||||||||
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References
- [1]. Wood N, et al. A liquid chromatographic-tandem mass spectrometric method for the determination of two selective thymidylate synthase inhibitors, BGC945 and BGC638, in mouse plasma. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2005 Sep 25;824(1-2):181-8.
- [2]. Gibbs DD, et al. BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors. Cancer research. 2005 Dec 15;65(24):11721-8. [Content Brief]
