Citarinostat (Synonyms: ACY241)

目录号: HY-15994 纯度: 99.30%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Citarinostat (ACY241) 是第二代有效的，口服活性，高选择性的 HDAC6 抑制剂，IC₅₀ 为 2.6 nM (HDAC1，HDAC2，HDAC3 和 HDAC8 的 IC₅₀ 分别为 35 nM，45 nM，46 nM 和 137 nM)。Citarinostat 具有抗癌作用。

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Citarinostat Chemical Structure

CAS No. : 1316215-12-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥772	In-stock
1 mg	￥449	In-stock
5 mg	￥750	In-stock
10 mg	￥1200	In-stock
25 mg	￥2450	In-stock
50 mg	￥4060	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献

Citarinostat 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HDAC 亚型特异性产品:

查看所有亚型

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

生物活性
纯度 & 产品资料
参考文献

生物活性

Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC₅₀ of 2.6 nM (IC₅₀s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects^[1].

IC₅₀ & Target^[1]

HDAC6

2.6 nM (IC₅₀)

HDAC1

35 nM (IC₅₀)

HDAC2

45 nM (IC₅₀)

HDAC3

46 nM (IC₅₀)

HDAC8

137 nM (IC₅₀)

HDAC7

7300 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BV-173	IC₅₀	0.9 μM Compound: Citarinostat	Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Fibroblast	IC₅₀	5.7 μM Compound: 6	Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	5.7 μM Compound: ACY-241	Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	5.74 μM Compound: ACY-241	Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Fibroblast	IC₅₀	7.4 μM Compound: 6	Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	7.4 μM Compound: ACY-241	Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	7.44 μM Compound: ACY-241	Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HeLa	IC₅₀	7 μM Compound: Citarinostat	Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
HuT78	IC₅₀	1.78 μM Compound: ACY-241	Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HUVEC	IC₅₀	4.86 μM Compound: ACY-241	Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HUVEC	IC₅₀	4.9 μM Compound: 6	Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
HUVEC	IC₅₀	4.9 μM Compound: ACY-241	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Jurkat	IC₅₀	1.2 μM Compound: Citarinostat	Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MM1.S	IC₅₀	1.52 μM Compound: 6	Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MM1.S	IC₅₀	1.6 μM Compound: Citarinostat	Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MM1.S	IC₅₀	1.61 μM Compound: ACY-241	Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
MOLM-13	IC₅₀	13.5 μM Compound: Citarinostat	Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MOLT-4	IC₅₀	1.72 μM Compound: ACY-241	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
MV4-11	IC₅₀	1.2 μM Compound: Citarinostat	Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MV4-11	IC₅₀	1.24 μM Compound: 6	Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MV4-11	IC₅₀	1.24 μM Compound: ACY-241	Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
MV4-11	IC₅₀	1.34 μM Compound: ACY-241	Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
MV4-11	IC₅₀	1.34 μM Compound: ACY-241	Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
NSC	IC₅₀	4.35 μM Compound: ACY-241	Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
OCI-AML-3	IC₅₀	7.7 μM Compound: Citarinostat	Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
RPMI-8226	IC₅₀	3.16 μM Compound: 6	Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
RPMI-8226	IC₅₀	6.5 μM Compound: Citarinostat	Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Sf9	IC₅₀	> 1 μM Compound: Citarinostat	Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.318 μM Compound: Citarinostat	Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	2.6 nM Compound: ACY-241	Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a	[PMID: 31414801]
Sf9	IC₅₀	35 nM Compound: ACY-241	Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr	[PMID: 31414801]
SU-DHL-1	IC₅₀	4.56 μM Compound: ACY-241	Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
U-87MG ATCC	IC₅₀	9.1 μM Compound: Citarinostat	Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]

体外研究
(In Vitro)

Citarinostat (ACY241;300 nM;24小时;A2780细胞)导致 α-微管蛋白高乙酰化增加，与微管蛋白去乙酰化酶 HDAC6 的抑制一致。Citarinostat低剂量可选择性抑制 HDAC6，而高剂量暴露可抑制 I 类 HDAC 同型酶^[1]。
Citarinostat 在 A2780、TOV-21G 卵巢癌和 MDA-MD-231 乳腺癌细胞中的IC₅₀ 范围为4.6 ~ 6.1 μM^[1]。
Citarinostat在 3 μM剂量下抑制细胞增殖，不诱导细胞凋亡，10 μM 时显著诱导细胞凋亡，完全抑制细胞增殖^[1]。

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

Western Blot Analysis^[1]

Cell Line:	A2780 cells
Concentration:	0 μM, 0.1 μM, 0.3 μM, 0.5μM, 1 μM, 3 μM
Incubation Time:	24 hours
Result:	Resulted in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, was only observed at doses above 1 μM.

体内研究
(In Vivo)

Citarinostat (ACY241；50 mg/kg；腹腔注射；每天一次，持续 5 天，随后停药两天；持续 3 周；雌性无胸腺裸鼠) 与 NSC 125973 联合使用显著抑制肿瘤生长^[1]。

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

Animal Model:	Female athymic nude mice (7-week-old) injected with TOV-21G cells^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks
Result:	Combination treatment with NSC 125973 resulted in significantly suppression of tumor growth.

Clinical Trial

分子量

467.95

Formula

C₂₄H₂₆ClN₅O₃

CAS 号

1316215-12-9

性状

固体

颜色

White to off-white

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 : ≥ 30 mg/mL (64.11 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	2.1370 mL	10.6849 mL	21.3698 mL
5 mM	0.4274 mL	2.1370 mL	4.2740 mL
10 mM	0.2137 mL	1.0685 mL	2.1370 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 (5.34 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: ≥ 2.5 mg/mL (5.34 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 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: ≥ 2.5 mg/mL (5.34 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，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 25.0 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: 99.30%

选择批次：

Data Sheet (639 KB) SDS (393 KB)

COA (282 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Huang P, et al. Selective HDAC inhibition by ACY-241 enhances the activity of NSC 125973 in solid tumor models. Oncotarget. 2017 Jan 10;8(2):2694-2707. [Content Brief]

Citarinostat 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	2.1370 mL	10.6849 mL	21.3698 mL	53.4245 mL
	5 mM	0.4274 mL	2.1370 mL	4.2740 mL	10.6849 mL
	10 mM	0.2137 mL	1.0685 mL	2.1370 mL	5.3425 mL
	15 mM	0.1425 mL	0.7123 mL	1.4247 mL	3.5616 mL
	20 mM	0.1068 mL	0.5342 mL	1.0685 mL	2.6712 mL
	25 mM	0.0855 mL	0.4274 mL	0.8548 mL	2.1370 mL
	30 mM	0.0712 mL	0.3562 mL	0.7123 mL	1.7808 mL
	40 mM	0.0534 mL	0.2671 mL	0.5342 mL	1.3356 mL
	50 mM	0.0427 mL	0.2137 mL	0.4274 mL	1.0685 mL
	60 mM	0.0356 mL	0.1781 mL	0.3562 mL	0.8904 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:

Citarinostat1316215-12-9ACY241ACY 241ACY-241HDACHistone deacetylasesHDAC6anticanceranti-proliferationα-tubulincombinationmultiple. myelomaInhibitorinhibitorinhibit

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Citarinostat (Synonyms: ACY241)

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Citarinostat (Synonyms: ACY241)

Customer Review

Citarinostat 相关抗体

MCE 顾客使用本产品发表的 3 篇科研文献

Citarinostat 相关产品

•相关化合物库:

•同靶点产品:

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查看 HDAC 亚型特异性产品:

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参考文献

Citarinostat 相关抗体:

摩尔计算器

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完整储备液配制表

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A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z