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Gemcitabine (Synonyms: 吉西他濱; LY 188011)
Gemcitabine (LY 188011) 是一種嘧啶核苷類似物抗代謝藥 (nucleoside antimetabolite/analog) 和抗腫瘤劑。Gemcitabine 抑制 DNA 合成 (DNA synthesis) 和修復，導致細胞自噬 (autophagy) 和凋亡 (apoptosis)。
生物活性
Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis
| IC50 & Target |
|---|
DNA synthesis[1]
體外研究(In Vitro)
Gemcitabine (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently[4].
Gemcitabine inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[4]
| Cell Line: | Non-senescent and replication-induced senescent new born dermal fibroblasts (NBFs) |
| Concentration: | 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM |
| Incubation Time: | 3 days |
| Result: | Killed replication-induced senescent NBFs for 3 days with 11.0% cell viability. |
體內(nèi)研究(In Vivo)
Gemcitabine can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg[2].
Treatment of the LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively)[3].
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00030745 | Swiss Group for Clinical Cancer Research | June 2000 | Phase 2 | |
| NCT00191347 | Eli Lilly and Company | October 2004 | Phase 2 | |
| NCT02583477 | AstraZeneca | March 25, 2016 | Phase 1|Phase 2 |
分子量：263.20
Formula：C9H11F2N3O4
CAS 號：95058-81-4
中文名稱：吉西他濱；雙氟脫氧胞苷
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
DMSO : 250 mg/mL (949.85 mM; Need ultrasonic)
Ethanol : 12.5 mg/mL (47.49 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.7994 mL | 18.9970 mL | 37.9939 mL |
| 5 mM | 0.7599 mL | 3.7994 mL | 7.5988 mL |
| 10 mM | 0.3799 mL | 1.8997 mL | 3.7994 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 0.5%HPMC 1%Tween80
Solubility: 20 mg/mL (75.99 mM); Clear solution; Need ultrasonic
- 3.
- 5.
- 6.
- 7.
- 8.
參考文獻
Gemcitabine (Synonyms: 吉西他濱; LY 188011)
Gemcitabine (LY 188011) 是一種嘧啶核苷類似物抗代謝藥 (nucleoside antimetabolite/analog) 和抗腫瘤劑。Gemcitabine 抑制 DNA 合成 (DNA synthesis) 和修復，導致細胞自噬 (autophagy) 和凋亡 (apoptosis)。
生物活性
Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis
| IC50 & Target |
|---|
DNA synthesis[1]
體外研究(In Vitro)
Gemcitabine (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently[4].
Gemcitabine inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[4]
| Cell Line: | Non-senescent and replication-induced senescent new born dermal fibroblasts (NBFs) |
| Concentration: | 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM |
| Incubation Time: | 3 days |
| Result: | Killed replication-induced senescent NBFs for 3 days with 11.0% cell viability. |
體內(nèi)研究(In Vivo)
Gemcitabine can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg[2].
Treatment of the LSL-KrasG12D/+; LSL-Trp53R172H; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively)[3].
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00030745 | Swiss Group for Clinical Cancer Research | June 2000 | Phase 2 | |
| NCT00191347 | Eli Lilly and Company | October 2004 | Phase 2 | |
| NCT02583477 | AstraZeneca | March 25, 2016 | Phase 1|Phase 2 |
分子量：263.20
Formula：C9H11F2N3O4
CAS 號：95058-81-4
中文名稱：吉西他濱；雙氟脫氧胞苷
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
DMSO : 250 mg/mL (949.85 mM; Need ultrasonic)
Ethanol : 12.5 mg/mL (47.49 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.7994 mL | 18.9970 mL | 37.9939 mL |
| 5 mM | 0.7599 mL | 3.7994 mL | 7.5988 mL |
| 10 mM | 0.3799 mL | 1.8997 mL | 3.7994 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 0.5%HPMC 1%Tween80
Solubility: 20 mg/mL (75.99 mM); Clear solution; Need ultrasonic
- 3.
- 5.
- 6.
- 7.
- 8.
參考文獻
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