AZD3965
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- CAS番号.
- 1448671-31-5
- 化学名:
- 别名:
- 英語名:
- AZD3965
- 英語别名:
- CS-2201;AZD-3965;AZD3965;AZD 3965;AZD3965,inhibit,Inhibitor,Monocarboxylate Transporter;(S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;5-{[(4S)-4-Hydroxy-4-methyl-1,2-oxazolidin-2-yl]carbonyl}-1-isopropyl-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;5-[[(4S)-4-Hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-
- CBNumber:
- CB63034312
- 化学式:
- C21H24F3N5O5S
- 分子量:
- 515.51
- MOL File:
- 1448671-31-5.mol
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AZD3965 物理性質
- 沸点 :
- 723.1±70.0 °C(Predicted)
- 比重(密度) :
- 1.483±0.06 g/cm3(Predicted)
- 貯蔵温度 :
- Store at -20°C
- 溶解性:
- insoluble in H2O; ≥51.5 mg/mL in DMSO; ≥51.6 mg/mL in EtOH
- 外見 :
- A crystalline solid
- 酸解離定数(Pka):
- 10.92±0.50(Predicted)
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
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| 注意喚起語 |
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| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H320 |
眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2B |
警告 |
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P264, P305+P351+P338,P337+P313 |
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| 注意書き |
| P264 |
取扱い後は皮膚をよく洗うこと。 |
| P264 |
取扱い後は手や顔をよく洗うこと。 |
| P305+P351+P338 |
眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
| P337+P313 |
眼の刺激が続く場合：医師の診断/手当てを受けること。 |
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AZD3965 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
AZD3965 化学特性,用途語,生産方法
説明
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; K
i = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport. It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 μM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts. AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.
酵素阻害剤
This orally bioavailable MCT1 inhibitor (FW = 515.51 g/mol; CASs =
733809-45-5 and 1448671-31-5), also named (S) -5- (4-hydroxy-4-
methylisoxazolidine-2-carbonyl) -1-isopropyl-3-methyl-6- ( (3-methyl-5- (tri-
fluoromethyl) -1H-pyrazol-4-yl) methyl) -thieno[2,3-d]pyrimidine-2,4 (1H,
3H) -dione, selectively targets the Monocarboxylate Transporter-1 (IC50 =
1.6 nM) and is ~6x less active toward MCT2. AZD3965 does not inhibit
MCT4, even at 10 μM. MCT1 and MCT4 are primarily involved in lactate
transport, targeting highly glycolytic cancer cells, especially those that are
hypoxic. The latter property suggests that the combined use with a
vascular-disrupting anticancer agent (such as combrestatin) may improve
the inhibitory action of AZD-3965 against cancer cells.
AZD3965 上流と下流の製品情報
原材料
準備製品
AZD3965 生産企業
Global( 78)Suppliers
- 1448671-31-5
- 5-[[(4S)-4-Hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- (S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- CS-2201
- AZD-3965;AZD3965;AZD 3965
- 5-{[(4S)-4-Hydroxy-4-methyl-1,2-oxazolidin-2-yl]carbonyl}-1-isopropyl-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-
- AZD3965,inhibit,Inhibitor,Monocarboxylate Transporter