JSH-150

目录号: HY-X0150 纯度: 98.03%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

JSH-150 是一种高效的选择性 CDK9 抑制剂， IC₅₀ 为 1 nM。

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JSH-150 Chemical Structure

CAS No. : 2247481-21-4

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可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1222	In-stock
1 mg	￥366	In-stock
5 mg	￥1100	In-stock
10 mg	￥1760	In-stock
25 mg	￥3340	In-stock
50 mg	￥4660	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

JSH-150 is a highly selective and potent CDK9 inhibitor with an IC₅₀ of 1 nM.

IC₅₀ & Target^[1]

CDK9/cyclinT1

1 nM (IC₅₀)

CDK16/Cyclin Y

292 nM (IC₅₀)

Cdk1/cyclin B

1.34 μM (IC₅₀)

CDK14/Cyclin Y

1.68 μM (IC₅₀)

CDK7/Cyclin H/MNAT1

1.72 μM (IC₅₀)

cdk2/cyclin A

2.86 μM (IC₅₀)

Cdk5/p25

4.64 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	GI₅₀	0.044 μM Compound: 40; JSH-150	Antiproliferative activity against human A375 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human A375 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
A-431	GI₅₀	0.019 μM Compound: 40; JSH-150	Antiproliferative activity against human A431 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human A431 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
CHO	GI₅₀	1.1 μM Compound: 40; JSH-150	Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against CHO cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
COLO 205	GI₅₀	0.014 μM Compound: 40; JSH-150	Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
GISTT1	GI₅₀	0.0021 μM Compound: 40; JSH-150	Antiproliferative activity against human GISTT1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human GISTT1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
HL-60	GI₅₀	0.056 μM Compound: 40; JSH-150	Antiproliferative activity against human HL60 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human HL60 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MOLM-13	GI₅₀	0.012 μM Compound: 40; JSH-150	Antiproliferative activity against human MOLM13 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MOLM13 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MOLM-14	GI₅₀	0.0011 μM Compound: 40; JSH-150	Antiproliferative activity against human MOLM14 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MOLM14 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
MV4-11	GI₅₀	0.012 μM Compound: 40; JSH-150	Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
OCI-AML-3	GI₅₀	0.0066 μM Compound: 40; JSH-150	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
Ramos	GI₅₀	0.013 μM Compound: 40; JSH-150	Antiproliferative activity against human Ramos cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human Ramos cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
SKM-1	GI₅₀	0.012 μM Compound: 40; JSH-150	Antiproliferative activity against human SKM1 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human SKM1 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
SK-N-BE(2)-M17	GI₅₀	0.034 μM Compound: 40; JSH-150	Antiproliferative activity against human BE(2)-M17 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human BE(2)-M17 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]
U-937	GI₅₀	0.002 μM Compound: 40; JSH-150	Antiproliferative activity against human U937 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human U937 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]

体外研究
(In Vitro)

JSH-150 在 A375 (黑色素瘤)、A431 (鳞状细胞)、BE (2) M17 (神经母细胞瘤)、GIST-T1 (GIST) 和 COLO205 (结肠癌) 等实体瘤细胞系中表现出有效的抗增殖活性， GI₅₀ 值从 0.002 到 0.044 μM。在急性髓性白血病 (AML)、慢性淋巴细胞白血病 (CLL) 和B细胞淋巴瘤细胞系等白血病细胞系中，JSH-150 也表现出较强的生长抑制作用，GI₅₀ 范围从单一到两位数 nM。此外，与癌细胞系相比，JSH-150 在正常 CHO 细胞 (GI₅₀：1.1 μM) 中的敏感性要低得多。

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

体内研究
(In Vivo)

以所有剂量 (即 10、20 和 30 mg/kg/天) 处理 JSH-150，在前两周几乎可以完全抑制肿瘤进展，并且不影响动物的体重，表明在这些阶段没有一般细胞毒性剂量。在停止JSH-150的处理后，用10mpk药物剂量处理的动物的肿瘤又开始生长。然而，在停止施用 JSH-150 后的下一周内，在 20 和 30 mpk 剂量组中未观察到这种肿瘤复发，并且在第 21 天量化 p 值，分别为 0.042、0.0035 和 0.0028。JSH-150 的药代动力学特性在不同物种中进行了评估，包括小鼠、Sprague-Dawley 大鼠和比格犬，通过静脉注射和口服给药。JSH-150在狗和小鼠中吸收迅速 (分别为T_max=1.33 h和2.00 h)，但在大鼠中吸收缓慢 (T_max=3.33 h)。JSH-150 在三个不同物种中的口服半衰期也不同 (小鼠 T_1/2=1.55 h，大鼠 3.37 h，犬 20.37 h)，表明它是与小鼠和大鼠相比，狗的代谢非常缓慢。此外，JSH-150 在小鼠、大鼠和狗中表现出可接受的生物利用度 (分别为 F=45.01%、45.10% 和 39.15%)。PK特性表明JSH-150适合口服给药^[1]。

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

分子量

505.08

Formula

C₂₄H₃₃ClN₆O₂S

CAS 号

2247481-21-4

性状

固体

颜色

Light yellow to yellow

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 : 100 mg/mL (197.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9799 mL	9.8994 mL	19.7988 mL
5 mM	0.3960 mL	1.9799 mL	3.9598 mL
10 mM	0.1980 mL	0.9899 mL	1.9799 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 (4.95 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 (4.95 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 (4.95 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: 98.36%

选择批次：

Data Sheet (652 KB) SDS (251 KB)

COA (260 KB) LCMS (101 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Beilei Wang, et al. Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor. Eur J Med Chem. 13 September 2018.

Cell Assay ^[1]	The A375 (melanoma), A431 (squamous), BE(2)M17 (neuroblastoma), BE(2)M17 (neuroblastoma), CRL-2234 (hepatoma), COLO205 (colon cancer), A549 (lung adenocarcinoma), Ramos (B cell lymphoma), MV4-11 (AML), Ramos (B cell lymphoma), U937 (AML), CHL (hamster lung cell), and CHO (hamster ovary cell) cell lines are used. OCI-AML-3 (AML), SKM-1 (AML), MEC-1 (CLL), MEC-2 (CLL) and HL-60 (human promyelocytic leukemia cells) are used. Human GIST-T1 cells are used. MOLM-13 and MOLM14 cell lines are used. All the cells are grown in a humidified incubator at 37°C under 5% CO2. A375, A431, GIST-T1, A549, Colo205 and CHO cells are maintained in DMEM supplemented with 10% FBS, 1% Penicillin/Streptomycin. BE(2)M17 cells are cultured with 1:1 mixture of ATCC-formulated Eagle's minimum essential medium, and F12 Medium. MV4-11, MEC-1 and MEC-2 are grown in IMDM supplemented with 10% FBS, 1% Penicillin/Streptomycin. CRL-2234, U2932, U937, Ramos, MOLM13, MOLM14, OCI-AML-3, SKM-1, HL-60 and CHL are grown in RPMI 1640 medium supported with 10% FBS and 1% Penicillin/Streptomycin. Adherent cells are grown in tissue culture flasks until they are 85-95% confluent prior to use. For suspension cells, cells are collected by spin down at 800 rpm/min for 5 min before use. Cells are grown in 96-well culture plates (3000 cells/well). The compounds (e.g., JSH-150) at various concentrations are added into the plates. Cell proliferation is determined after treatment with compounds (e.g., JSH-150) for 72 h. Cell viability is measured using the Cell Titer-Glo assay and luminescence is measured in a multilabel reader^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Five-week-old female nu/nu mice are used. Prior to implantation, cells are harvested during exponential growth. Five million MV4-11 cells in PBS are formulated as a 1:1 mixture with Matrigel and injected into the subcutaneous space on the right flank of nu/nu mice. Daily oral administration is initiated when MV4-11 tumors have reached a size of 200-400 mm³. Animals are then randomized into treatment groups of 5 mice each for efficacy studies. JSH-150 is delivered daily in a HKI solution (0.5% methocellulose/0.4% Tween80 in ddH₂O) by oral gavage. A range of doses of JSH-150 or its vehicle as control are administered. Female nu/nu mice bearing established MV4-11 tumor xenografts are treated with JSH-150 at 10, 20, and 30 mg/kg/d dosage or vehicle. Body weight is measured daily and tumor growth is measured every day after JSH-150 treatment. Tumor volume is calculated^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Beilei Wang, et al. Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor. Eur J Med Chem. 13 September 2018.

JSH-150 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	1.9799 mL	9.8994 mL	19.7988 mL	49.4971 mL
	5 mM	0.3960 mL	1.9799 mL	3.9598 mL	9.8994 mL
	10 mM	0.1980 mL	0.9899 mL	1.9799 mL	4.9497 mL
	15 mM	0.1320 mL	0.6600 mL	1.3199 mL	3.2998 mL
	20 mM	0.0990 mL	0.4950 mL	0.9899 mL	2.4749 mL
	25 mM	0.0792 mL	0.3960 mL	0.7920 mL	1.9799 mL
	30 mM	0.0660 mL	0.3300 mL	0.6600 mL	1.6499 mL
	40 mM	0.0495 mL	0.2475 mL	0.4950 mL	1.2374 mL
	50 mM	0.0396 mL	0.1980 mL	0.3960 mL	0.9899 mL
	60 mM	0.0330 mL	0.1650 mL	0.3300 mL	0.8250 mL
	80 mM	0.0247 mL	0.1237 mL	0.2475 mL	0.6187 mL
	100 mM	0.0198 mL	0.0990 mL	0.1980 mL	0.4950 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:

JSH-1502247481-21-4JSH150JSH 150CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

JSH-150

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