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Verteporfin (Synonyms: 維替泊芬; CL 318952)
Verteporfin (CL 318952) 是一種用于光動力療法的光敏劑，用于消除與年齡相關(guān)的黃斑變性等疾病相關(guān)的眼內(nèi)異常血管。 Verteporfin 是一種 YAP 抑制劑，可破壞 YAP-TEAD 相互作用。Verteporfin 可以誘導(dǎo)細(xì)胞凋亡 (apoptosis)。Verteporfin 是一種自噬 (autophagy) 抑制劑，通過抑制自噬小體形成，在早期阻斷自噬。
生物活性
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis[1]. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation[3].
IC50 & Target：IC50: YAP-TEAD interaction
體外研究(In Vitro)
Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 μM, 2.11 μM, and 5.61 μM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells[1]. Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and NSC 125973 shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T[2].
體內(nèi)研究(In Vivo)
Verteporfin (10 mg/kg, c.s.c.) and BMS-354825 significantly reduces the leukemia cell ratio, and combined therapy further reduced the number of leukemia cells in the spleen[1].
分子量：718.79
Formula：C82H84N8O16
CAS 號：129497-78-5
中文名稱：維替泊芬
運(yùn)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)
In Vitro:
DMF : 25 mg/mL (34.78 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3912 mL | 6.9561 mL | 13.9123 mL |
| 5 mM | 0.2782 mL | 1.3912 mL | 2.7825 mL |
| 10 mM | 0.1391 mL | 0.6956 mL | 1.3912 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(fù)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?jiān)?6 個月內(nèi)使用，-20°C 儲存時，請?jiān)?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(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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
- 2.
請依序添加每種溶劑： 10% DMF 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (3.48 mM); Suspended solution; Need ultrasonic
- 3.
參考文獻(xiàn)
在線客服客服一Verteporfin (Synonyms: 維替泊芬; CL 318952)
Verteporfin (CL 318952) 是一種用于光動力療法的光敏劑，用于消除與年齡相關(guān)的黃斑變性等疾病相關(guān)的眼內(nèi)異常血管。 Verteporfin 是一種 YAP 抑制劑，可破壞 YAP-TEAD 相互作用。Verteporfin 可以誘導(dǎo)細(xì)胞凋亡 (apoptosis)。Verteporfin 是一種自噬 (autophagy) 抑制劑，通過抑制自噬小體形成，在早期阻斷自噬。
生物活性
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis[1]. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation[3].
IC50 & Target：IC50: YAP-TEAD interaction
體外研究(In Vitro)
Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 μM, 2.11 μM, and 5.61 μM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells[1]. Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and NSC 125973 shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T[2].
體內(nèi)研究(In Vivo)
Verteporfin (10 mg/kg, c.s.c.) and BMS-354825 significantly reduces the leukemia cell ratio, and combined therapy further reduced the number of leukemia cells in the spleen[1].
分子量：718.79
Formula：C82H84N8O16
CAS 號：129497-78-5
中文名稱：維替泊芬
運(yùn)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)
In Vitro:
DMF : 25 mg/mL (34.78 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3912 mL | 6.9561 mL | 13.9123 mL |
| 5 mM | 0.2782 mL | 1.3912 mL | 2.7825 mL |
| 10 mM | 0.1391 mL | 0.6956 mL | 1.3912 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(fù)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?jiān)?6 個月內(nèi)使用，-20°C 儲存時，請?jiān)?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(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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
- 2.
請依序添加每種溶劑： 10% DMF 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (3.48 mM); Suspended solution; Need ultrasonic
- 3.
參考文獻(xiàn)
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