LY243246
LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis.
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- CAS 番号: 106400-18-4
- 分子式: C21H25N5O6
- 分子量:443.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
LY243246 ((6S)-DDATHF) is a growth inhibitor of mouse L1210 leukemia cells (IC50=29 nM). Both diastereomers of DDATHF are found to be efficient substrates for folylpolyglutamate synthetase of both mouse and human origin (6R- and 6S-diastereomers of DDATHF: Km=7.1 and 9.3 μM for mouse liver folylpolyglutamate synthetase, respectively)[1].
Both the 6R and 6S diastereomers of DDATHF are also cytotoxic to mammalian cells in a stereospecific manner. The cytotoxic potency of (6R)-DDATHF towards different cell lines varied by approximately 14-fold and that of (6S)-DDATHF by as much as 156-fold. Compared to (6R)-DDATHF, (6S)-DDATHF is 6.0- and 7.2-fold more cytotoxic to human WiDr colon adenocarcinoma and Chinese hamster ovary (CHO) cells, respectively, and only 1.5- and 2.0-fold more cytotoxic to human T24 bladder carcinoma and mouse L1210 leukemia cells, respectively. However, compared to (6S)-DDATHF, (6R)-DDATHF was 8.7- and 6.9-fold more cytotoxic to C3H/10T1/2 clone 8 and clone 16 mouse fibroblasts, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 106400-18-4
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分子量 443.45
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分子式 C21H25N5O6
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(CC[C@H](CN2)CC3=C2NC(N)=NC3=O)C=C1)=O
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別名
(6S)-DDATHF
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Moran RG, et al. The 6S- and 6R-diastereomers of 5, 10-dideaza-5, 6, 7, 8-tetrahydrofolate are equiactive inhibitors of de novo purine synthesis. J Biol Chem. 1989;264(35):21047-21051. [Content Brief]
[2]. Lehman NL. The stereospecific cytotoxic potency of (6R) and (6S)-5,10- dideazatetrahydrofolate correlates with cellular folylpolyglutamate synthetase levels. Biochimie. 1995;77(4):273-278. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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