Gemcitabine elaidate hydrochloride CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5'-elaidate hydrochloride|西域试剂

Gemcitabine elaidate hydrochloride CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5'-elaidate hydrochloride,97.0%

产品编号：Bellancom-13538A| 分子式：C₂₇H₄₄ClF₂N₃O₅| 分子量：564.11

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货号	价格	库存与货期
Bellancom-13538A	￥1050.00	杭州北京（现货）
Bellancom-13538A	￥1450.00	杭州北京（现货）
Bellancom-13538A	￥4450.00	杭州北京（现货）
Bellancom-13538A	￥6680.00	杭州北京（现货）

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Gemcitabine elaidate hydrochloride CP-4126 hydrochloride; CO-101 hydrochloride; Gemcitabine 5'-elaidate hydrochloride

产品介绍

Gemcitabine elaidate (CP-4126) hydrochloride 是 Gemcitabine 的亲脂性前体。Gemcitabine elaidate hydrochloride 通过酯酶转化为 Gemcitabine 以被磷酸化。Gemcitabine elaidate hydrochloride 具有抗肿瘤活性。

生物活性

Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity.

体外研究

Gemcitabine elaidate (0.2 nM-1 mM; 72 h) hydrochloride inhibits the growth of gemcitabine sensitive and resistant cells, with IC₅₀s of 0.0033, 16.0, 0.0042, 13.0, 0.0015, 0.03, 0.0025, 91, 0.0040, 0.0077, 0.028, and 0.088 μM for L1210/L5, L4A6, BCLO, Bara-C, C26-A, C26-G, A2780, AG6000, THX, LOX, MOLT4 and MOLT4/C8 cells, respectively.
Gemcitabine elaidate (0.5 nM-1 μM; 72 h) hydrochloride increases S phase accumulation and dose-dependent cell kill in A549 and WiDR cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

Cell Line:	A549 and WiDR cells
Concentration:	0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1.0 μM
Incubation Time:	72 h
Result:	Induced a G2/M and S phase accumulation.

体内研究
(In Vivo)

Gemcitabine elaidate (25-120 mg/kg; i.p. every 3 days for 5 doses) hydrochloride inhibits the solid tumor xenografts growth of non-small cell lung cancer (EKVX), non-classifiable sarcoma (MHMX), fibrous histiocytoma (TAX II-1), malignant melanoma (THX), prostate cancer (CRL-1435), pancreatic cancer (PANC-1).
Gemcitabine elaidate (10-20 mg/kg; p.o. every 3 days for 5 doses) hydrochloride shows acceptable toxicity and significant antitumor activity in the colon cancer xenograft Co6044 bearing mice.
Gemcitabine elaidate (p.o. once daily for 5 doses) hydrochloride shows a favorable toxicity and antitumor activity, while the dose of 15 mg/kg is highly toxic in the human colon cancer xenograft Co6044.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively
Dosage:	25-120 mg/kg
Administration:	I.p. every 3 days for 5 doses
Result:	Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively
Dosage:	25-120 mg/kg
Administration:	I.p. every 3 days for 5 doses
Result:	Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c nude (nu/nu) mice (5-8 weeks; 20-27 g) were bearing tumor of EKVX, H-146, MHMX, TAX II-1, OHS, THX, MA-11, CRL-1435, PANC-1 and MiaPaCa-2, respectively
Dosage:	25-120 mg/kg
Administration:	I.p. every 3 days for 5 doses
Result:	Inhibited the growth of EKVX, MHMX, TAX II-1, THX, CRL-1435 and PANC-1, with T/C values of 7%, 1%, 30%, 7%, 9%, and 12%, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (177.27 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7727 mL	8.8635 mL	17.7270 mL
5 mM	0.3545 mL	1.7727 mL	3.5454 mL
10 mM	0.1773 mL	0.8864 mL	1.7727 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。