Raltitrexed (Synonyms: 雷替曲塞; ZD1694; D1694; ICI-D1694)

目录号: HY-10821 纯度: 99.49%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Raltitrexed是一种用于化疗的抗代谢活性分子，通过抑制胸苷酸合成酶起作用。

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Raltitrexed Chemical Structure

CAS No. : 112887-68-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥363	In-stock
5 mg	￥291	In-stock
10 mg	￥515	In-stock
25 mg	￥948	In-stock
50 mg	￥1613	In-stock
100 mg	￥2813	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

MCE 顾客使用本产品发表的 8 篇科研文献

Raltitrexed 相关产品

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•同靶点产品:

•同靶点蛋白产品:

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase.

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	4.68 μM Compound: RTX	Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
A549	IC₅₀	0.81 μM Compound: RTX	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
HCT-116	IC₅₀	0.076 μM Compound: RTX	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
HeLa	IC₅₀	5.51 μM Compound: RTX	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
HepG2	IC₅₀	1.3 μM Compound: Raltitrexed, ZD1694	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 23490159]
HepG2	IC₅₀	9.63 μM Compound: RTX	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
IGROV-1	IC₅₀	12.6 nM Compound: RTX, ZD-1694	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
IGROV-1	IC₅₀	20 nM Compound: RTX, ZD-1694	Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human IGROV1 cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
KB	IC₅₀	22 nM Compound: RTX	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	22 nM Compound: RTX, raltitrexed	Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid	[PMID: 24111942]
KB	IC₅₀	22 nM Compound: RTX	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs in presence of 200 nM folic acid by Celltiter-blue cell viability assay	[PMID: 25234128]
KB	IC₅₀	22 nM Compound: RTX, ZD-1694	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs in the presence of 200 nM folic acid	[PMID: 21879757]
KB	IC₅₀	5.9 nM Compound: RTX	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	5.9 nM Compound: RTX, raltitrexed	Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
KB	IC₅₀	5.9 nM Compound: RTX, ZD-1694	Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
KB	IC₅₀	5.9 nM Compound: RTX	Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
MCF-10A	IC₅₀	> 20 μM Compound: RTX	Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MCF7	IC₅₀	10.9 μM Compound: RTX	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MCF7	IC₅₀	12.6 μM Compound: Raltitrexed, ZD1694	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23490159]
MDA-MB-231	IC₅₀	> 20 μM Compound: RTX	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
MGC-803	IC₅₀	9.52 μM Compound: RTX	Cytotoxicity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]
R2	IC₅₀	> 1000 nM Compound: RTX, ZD-1694	Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
R2	IC₅₀	> 1000 nM Compound: RTX	Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	> 1000 nM Compound: RTX	Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay Cytotoxicity against Chinese hamster R2 cells expressing empty vector assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay	[PMID: 25234128]
R2	IC₅₀	15 nM Compound: RTX	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
R2	IC₅₀	15 nM Compound: RTX	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis	[PMID: 27458733]
R2	IC₅₀	99.5 nM Compound: RTX, raltitrexed	Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
R2	IC₅₀	99.5 nM Compound: RTX	Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay	[PMID: 24256410]
R2	IC₅₀	99.5 nM Compound: RTX, ZD-1694	Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as reduction of viable cells after 96 hrs	[PMID: 21879757]
SGC-7901	IC₅₀	8.7 μM Compound: Raltitrexed, ZD1694	Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay Cytotoxicity against human SGC7901 cells after 48 hrs by MTT assay	[PMID: 23490159]
U2OS	IC₅₀	> 20 μM Compound: RTX	Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36331508]

体外研究
(In Vitro)

Raltitrexed inhibits HepG2 proliferation by arresting the cell cycle at G0/G1, and the cell cycle is mediated via downregulation of cyclin A and CDK2^[1]. Raltitrexed (0.1, 0.5, 2.5 μg/mL) decreases the viability of SGC7901 cells in a dose- and time-dependent manner. Raltitrexed (0.5 μg/mL) shows typical apoptotic morphology, including nuclear shrinkage, fragmentation, chromatin condensation and apoptotic bodies in SGC7901 cells. Raltitrexed blocks the cell cycle at the G0/G1 phase, decreases in the mitochondrial membrane potential. Raltitrexed also increases the level of ROS, induces caspase-3-dependent apoptosis via activation of the mitochondria, and increases TS protein and mRNA expression levels^[3]. Raltitrexed (1.5 nM) reduces the number of GM00637 cells, selectively induces gene conversions, but does not affect DSB-induced HR or NHEJ^[4].

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

体内研究
(In Vivo)

Raltitrexed (0, 5, 10, 11.5, 13.5, 15 mg/kg b/w, i.p.) increases the rates of resorbed embryos and growth retardation of murine model of NTDs in a dose dependent manner. Raltitrexed (11.5 mg/kg b/w) maximally inhibits the thymidylate synthase (TS) activity in embryonic tissue, decreases dTMP levels and while increases dUMP levels^[2].

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

Clinical Trial

分子量

458.49

Formula

C₂₁H₂₂N₄O₆S

CAS 号

112887-68-0

性状

固体

颜色

Off-white to yellow

中文名称

雷替曲塞；雷替曲噻

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 29 mg/mL (63.25 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1811 mL	10.9054 mL	21.8107 mL
5 mM	0.4362 mL	2.1811 mL	4.3621 mL
10 mM	0.2181 mL	1.0905 mL	2.1811 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.45 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.54 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.54 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.49%

选择批次：

Data Sheet (630 KB) SDS (643 KB)

COA (195 KB) HNMR (266 KB) LCMS (265 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zhao H, et al. Raltitrexed Inhibits HepG2 Cell Proliferation via G0/G1 Cell Cycle Arrest. Oncol Res. 2016;23(5):237-48 [Content Brief]

[2]. Dong Y, et al. Raltitrexed's effect on the development of neural tube defects in mice is associated with DNA damage, apoptosis, and proliferation. Mol Cell Biochem. 2015 Jan;398(1-2):223-31. [Content Brief]

[3]. Xue S, et al. Raltitrexed induces mitochondrial-mediated apoptosis in SGC7901 human gastric cancer cells. Mol Med Rep. 2014 Oct;10(4):1927-34. [Content Brief]

[4]. Waldman BC, et al. Induction of intrachromosomal homologous recombination in human cells by raltitrexed, an inhibitor of thymidylate synthase. DNA Repair (Amst). 2008 Oct 1;7(10):1624-35. [Content Brief]

Cell Assay ^[4]	To assess the effect of Raltitrexed on cell viability and/or growth, GM00637 cells are plated into 25 cm² flasks at a density of 3.3×10⁵ cells per flask. Twenty four hours later, the medium is replaced with medium supplemented with various doses of Raltitrexed over a broad range of concentrations ranging from less than 1 nM to greater than 1 µM. Three flasks of cells are used for each dose tested. Cells are exposed to Raltitrexed for 24 hours, at which time the cells are refed with medium containing no Raltitrexed. Forty-eight hours after feeding with drug-free medium, cells are harvested and counted. The cell counts for the cells exposed to the various Raltitrexed doses are compared with the cell count for control cells not exposed to Raltitrexed as a measure of the impact of Raltitrexed on cell viability and/or growth rate. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	The adult (7-8 week, 19-20 g) C57BL/6 mice are used in the experiment. Mice are maintained under 22°C with a 12 h light/day cycle and fed with standard mouse chow and tap water ad libitum. Female mice are mated with male overnight and vaginal plugs are examined in the following morning. The presence of vaginal plug in the pregnant mice is considered as gestational day 0.5. Pregnant mice are randomly divided into 6 groups with 10 mice in each group. Raltitrexed is dissolved in 0.9 % NaCl, and five groups are intraperitoneally injected with different doses of Raltitrexed (5, 10, 11.5, 13.5, 15 mg/kg b/w) on gestational day 7.5. The control group is intraperitoneally injected with 0.9 % NaCl at the same volume on gestational day 7.5. On gestational day 11.5, pregnant mice are sacrificed, and embryos are examined under dissect microscope. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Zhao H, et al. Raltitrexed Inhibits HepG2 Cell Proliferation via G0/G1 Cell Cycle Arrest. Oncol Res. 2016;23(5):237-48 [Content Brief] [2]. Dong Y, et al. Raltitrexed's effect on the development of neural tube defects in mice is associated with DNA damage, apoptosis, and proliferation. Mol Cell Biochem. 2015 Jan;398(1-2):223-31. [Content Brief] [3]. Xue S, et al. Raltitrexed induces mitochondrial-mediated apoptosis in SGC7901 human gastric cancer cells. Mol Med Rep. 2014 Oct;10(4):1927-34. [Content Brief] [4]. Waldman BC, et al. Induction of intrachromosomal homologous recombination in human cells by raltitrexed, an inhibitor of thymidylate synthase. DNA Repair (Amst). 2008 Oct 1;7(10):1624-35. [Content Brief]

Raltitrexed 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1811 mL	10.9054 mL	21.8107 mL	54.5268 mL
	5 mM	0.4362 mL	2.1811 mL	4.3621 mL	10.9054 mL
	10 mM	0.2181 mL	1.0905 mL	2.1811 mL	5.4527 mL
	15 mM	0.1454 mL	0.7270 mL	1.4540 mL	3.6351 mL
	20 mM	0.1091 mL	0.5453 mL	1.0905 mL	2.7263 mL
	25 mM	0.0872 mL	0.4362 mL	0.8724 mL	2.1811 mL
	30 mM	0.0727 mL	0.3635 mL	0.7270 mL	1.8176 mL
	40 mM	0.0545 mL	0.2726 mL	0.5453 mL	1.3632 mL
	50 mM	0.0436 mL	0.2181 mL	0.4362 mL	1.0905 mL
	60 mM	0.0364 mL	0.1818 mL	0.3635 mL	0.9088 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Raltitrexed112887-68-0ZD1694 D1694 ICI-D1694雷替曲塞雷替曲噻ZD 1694ZD-1694D1694D 1694D-1694Thymidylate SynthaseNucleoside Antimetabolite/AnalogInhibitorinhibitorinhibit

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Raltitrexed (Synonyms: 雷替曲塞; ZD1694; D1694; ICI-D1694)

MCE 顾客使用本产品发表的 8 篇科研文献

Raltitrexed 相关产品

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•同靶点产品:

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生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Raltitrexed 相关分类

完整储备液配制表

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Raltitrexed (Synonyms: 雷替曲塞; ZD1694; D1694; ICI-D1694)

Raltitrexed 相关抗体

MCE 顾客使用本产品发表的 8 篇科研文献

Raltitrexed 相关产品

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生物活性

实验参考方法

纯度 & 产品资料

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Raltitrexed 相关抗体:

摩尔计算器

稀释计算器

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