5-Fluorouracil (5-氟脲嘧啶; 5-FU)

5-Fluorouracil (5-FU) 是一種尿嘧啶的類似物 (nucleoside antimetabolite/analog)，是一種有效的抗腫L藥。5-Fluorouracil 通過抑制胸苷酸合成酶影響嘧啶的合成，從而耗盡細(xì)胞內(nèi)dTTP 池。5-Fluorouracil 誘導(dǎo)細(xì)胞凋亡 (apoptosis)，可用作化學(xué)敏化劑。5-Fluorouracil 還可抑制 HIV 病毒。5-Fluorouracil (5-FU) 可破壞外泌體特異性的 rRNA。
編號：HY-90006 ，CAS： 51-21-8

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號： HY-90006

起訂量：1

規(guī)格:：5g

價格:：￥840

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產(chǎn)品詳情

5-Fluorouracil (Synonyms: 5-氟脲嘧啶; 5-FU)

5-Fluorouracil (5-FU) 是一種尿嘧啶的類似物 (nucleoside antimetabolite/analog)，是一種有效的抗腫L藥。5-Fluorouracil 通過抑制胸苷酸合成酶影響嘧啶的合成，從而耗盡細(xì)胞內(nèi)dTTP 池。5-Fluorouracil 誘導(dǎo)細(xì)胞凋亡 (apoptosis)，可用作化學(xué)敏化劑。5-Fluorouracil 還可抑制 HIV 病毒。5-Fluorouracil (5-FU) 可破壞外泌體特異性的 rRNA。

生物活性

5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer^[1]^[2]. 5-Fluorouracil also inhibits HIV^[3].

IC₅₀ & Target^[1]^[6]

Human Endogenous Metabolite

HIV

體外研究(In Vitro)

5-Fluorouracil (5-Fu) and NSC 123127 (Dox) show synergistic anticancer efficacy. The IC₅₀ value of 5-Fu/Dox-DNM toward human breast cancer (MDA-MB-231) cells is 0.25 μg/mL, presenting an 11.2-fold and 6.1-fold increase in cytotoxicity compared to Dox-DNM and 5-Fu-DNM, respectively^[1]. In 5-fluorouracil (5-FU) and CDDP treated NFBD1-inhibited NPC cells, the NFBD1 expression in NPC CNE1 cell lines is depleted using lentivirus-mediated short hairpin RNA, and the sensitivity of these cells is elevated. NFBD1 knockdown leads to an obvious induction of apoptosis in CDDP- or 5-FU-treated CNE1 cells^[2].

體內(nèi)研究(In Vivo)

5-Fluorouracil (23 mg/kg, 3 times/week) for 14 days, induces accelerated gastrointestinal transit associated with acute intestinal inflammation at day 3 after the start of treatment, which may have led to persistent changes in the ENS observed after days 7 and 14 of treatment contributing to delayed gastrointestinal transit and colonic dysmotility^[4].

分子量：130.08

Formula：C₄H₃FN₂O₂

CAS 號：51-21-8

中文名稱：5-氟脲嘧啶；雙喃呋啶

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:

DMSO : 100 mg/mL (768.76 mM; Need ultrasonic)

H₂O : 20 mg/mL (153.75 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	7.6876 mL	38.4379 mL	76.8758 mL
5 mM	1.5375 mL	7.6876 mL	15.3752 mL
10 mM	0.7688 mL	3.8438 mL	7.6876 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，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

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

1.

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution
2.

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution
3.

請依序添加每種溶劑： 5% DMSO 95% saline
Solubility: 2.5 mg/mL (19.22 mM); Clear solution; Need ultrasonic

參考文獻(xiàn)

[1]. Han R, et al. Amphiphilic dendritic nanomicelle-mediated co-delivery of 5-fluorouracil and NSC 123127 for enhanced therapeutic efficacy. J Drug Target. 2016 Jun 29:1-28. [Epub ahead of print]

[2]. Zeng Q, et al. Knockdown of NFBD1/MDC1 enhances chemosensitivity to NSC 119875 or 5-fluorouracil in nasopharyngeal carcinoma CNE1 cells. Mol Cell Biochem. 2016 Jul;418(1-2):137-46.

[3]. Jones DH, et al. Ten-Year and Beyond Follow-up After Treatment With Highly Purified Liquid-Injectable Silicone for HIV-Associated Facial Lipoatrophy: A Report of 164 Patients. Dermatol Surg. 2019 Jul;45(7):941-948.

[4]. McQuade RM, et al. Gastrointestinal dysfunction and enteric neurotoxicity following treatment with anticancer chemotherapeutic agent 5-fluorouracil. Neurogastroenterol Motil. 2016 Jun 28.

[5]. Yin L, et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer in vitro and in vivo. Ther Clin Risk Manag. 2017 Feb 7;13:117-130.

[6]. Snyder SM, et al. Initial Experience with Topical Fluorouracil for Treatment of HIV-Associated Anal Intraepithelial Neoplasia. J Int Assoc Physicians AIDS Care (Chic). 2011;10(2):83-88.

[7]. Pek Yee Lum, et al. Discovering modes of action for therapeutic compounds using a genome-wide screen of yeast heterozygotes. Cell. 2004 Jan 9;116(1):121-37.

5-Fluorouracil (5-氟脲嘧啶; 5-FU)

5-Fluorouracil (5-FU) 是一種尿嘧啶的類似物 (nucleoside antimetabolite/analog)，是一種有效的抗腫L藥。5-Fluorouracil 通過抑制胸苷酸合成酶影響嘧啶的合成，從而耗盡細(xì)胞內(nèi)dTTP 池。5-Fluorouracil 誘導(dǎo)細(xì)胞凋亡 (apoptosis)，可用作化學(xué)敏化劑。5-Fluorouracil 還可抑制 HIV 病毒。5-Fluorouracil (5-FU) 可破壞外泌體特異性的 rRNA。
編號：HY-90006 ，CAS： 51-21-8

品牌：MCE

型號： HY-90006

起訂量：1

規(guī)格:：5g

價格:：￥840

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產(chǎn)品詳情

5-Fluorouracil (Synonyms: 5-氟脲嘧啶; 5-FU)

5-Fluorouracil (5-FU) 是一種尿嘧啶的類似物 (nucleoside antimetabolite/analog)，是一種有效的抗腫L藥。5-Fluorouracil 通過抑制胸苷酸合成酶影響嘧啶的合成，從而耗盡細(xì)胞內(nèi)dTTP 池。5-Fluorouracil 誘導(dǎo)細(xì)胞凋亡 (apoptosis)，可用作化學(xué)敏化劑。5-Fluorouracil 還可抑制 HIV 病毒。5-Fluorouracil (5-FU) 可破壞外泌體特異性的 rRNA。

生物活性

5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer^[1]^[2]. 5-Fluorouracil also inhibits HIV^[3].

IC₅₀ & Target^[1]^[6]

Human Endogenous Metabolite

HIV

體外研究(In Vitro)

5-Fluorouracil (5-Fu) and NSC 123127 (Dox) show synergistic anticancer efficacy. The IC₅₀ value of 5-Fu/Dox-DNM toward human breast cancer (MDA-MB-231) cells is 0.25 μg/mL, presenting an 11.2-fold and 6.1-fold increase in cytotoxicity compared to Dox-DNM and 5-Fu-DNM, respectively^[1]. In 5-fluorouracil (5-FU) and CDDP treated NFBD1-inhibited NPC cells, the NFBD1 expression in NPC CNE1 cell lines is depleted using lentivirus-mediated short hairpin RNA, and the sensitivity of these cells is elevated. NFBD1 knockdown leads to an obvious induction of apoptosis in CDDP- or 5-FU-treated CNE1 cells^[2].

體內(nèi)研究(In Vivo)

5-Fluorouracil (23 mg/kg, 3 times/week) for 14 days, induces accelerated gastrointestinal transit associated with acute intestinal inflammation at day 3 after the start of treatment, which may have led to persistent changes in the ENS observed after days 7 and 14 of treatment contributing to delayed gastrointestinal transit and colonic dysmotility^[4].

分子量：130.08

Formula：C₄H₃FN₂O₂

CAS 號：51-21-8

中文名稱：5-氟脲嘧啶；雙喃呋啶

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:

DMSO : 100 mg/mL (768.76 mM; Need ultrasonic)

H₂O : 20 mg/mL (153.75 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	7.6876 mL	38.4379 mL	76.8758 mL
5 mM	1.5375 mL	7.6876 mL	15.3752 mL
10 mM	0.7688 mL	3.8438 mL	7.6876 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，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

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

1.

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution
2.

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (19.22 mM); Clear solution
3.

請依序添加每種溶劑： 5% DMSO 95% saline
Solubility: 2.5 mg/mL (19.22 mM); Clear solution; Need ultrasonic