PIM1-IN-1

目录号: HY-111552 纯度: 99.83%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

PIM1-IN-1 是一种有效、高度选择性的 PIM1/3 抑制剂，对 PIM1，PIM2 和 PIM3 的 IC₅₀ 值分别为 7，5530 和 70 nM。PIM1-IN-1 抑制 PIM 下游蛋白 BAD 的磷酸化，EC₅₀ 值为 262 nM，而对 FLT3 或 hERG 无作用。具有抗增殖、抗肿瘤作用。

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PIM1-IN-1 Chemical Structure

CAS No. : 1417630-95-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4180	In-stock
1 mg	￥1727	In-stock
5 mg	￥3800	In-stock
10 mg	￥6000	In-stock
50 mg		询价
100 mg		询价

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PIM1-IN-1 相关产品

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PIM1 PIM2 PIM3

生物活性
纯度 & 产品资料
参考文献

生物活性

PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC₅₀s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC₅₀ of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity^[1].

IC₅₀ & Target^[1]

PIM1

7 nM (IC₅₀)

PIM3

70 nM (IC₅₀)

PIM2

5530 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	GI₅₀	21.8 μM Compound: 42	Antiproliferative activity against human A375 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A375 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
A498	GI₅₀	8.98 μM Compound: 42	Antiproliferative activity against human A498 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A498 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
A549	GI₅₀	16.2 μM Compound: 42	Antiproliferative activity against human A549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
A673	GI₅₀	12.7 μM Compound: 42	Antiproliferative activity against human A673 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human A673 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
ASPC1	GI₅₀	7.25 μM Compound: 42	Antiproliferative activity against human Aspc-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Aspc-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
BT-549	GI₅₀	20.4 μM Compound: 42	Antiproliferative activity against human BT549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human BT549 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
BXPC-3	GI₅₀	9.21 μM Compound: 42	Antiproliferative activity against human BxPC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human BxPC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
CAKI-1	GI₅₀	22.1 μM Compound: 42	Antiproliferative activity against human CAKI-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human CAKI-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
COLO 205	GI₅₀	5.25 μM Compound: 42	Antiproliferative activity against human COLO205 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human COLO205 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
DU-145	GI₅₀	22.4 μM Compound: 42	Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HCT-116	GI₅₀	21.2 μM Compound: 42	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
HL-60	GI₅₀	13.6 μM Compound: 42	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
JeKo-1	GI₅₀	7.3 μM Compound: 42	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
K562	GI₅₀	19.9 μM Compound: 42	Antiproliferative activity against human K562 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human K562 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
LNCaP	GI₅₀	18.6 μM Compound: 42	Antiproliferative activity against human LNCAP cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human LNCAP cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MCF7	GI₅₀	19.6 μM Compound: 42	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MDA-MB-231	GI₅₀	21.2 μM Compound: 42	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MIA PaCa-2	GI₅₀	17.4 μM Compound: 42	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
MV4-11	GI₅₀	6.46 μM Compound: 42	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NAMALVA	GI₅₀	9.68 μM Compound: 42	Antiproliferative activity against human NAMALWA cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human NAMALWA cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H1299	EC₅₀	262 nM Compound: 42	Inhibition of PIM1 in human NCI-H1299 cells assessed as reduction in BAD phosphorylation at Ser-112 residue incubated for 4 hrs by ELISA Inhibition of PIM1 in human NCI-H1299 cells assessed as reduction in BAD phosphorylation at Ser-112 residue incubated for 4 hrs by ELISA	[PMID: 30802730]
NCI-H1650	GI₅₀	22.5 μM Compound: 42	Antiproliferative activity against human NCI-H1650 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human NCI-H1650 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
NCI-H522	GI₅₀	9.7 μM Compound: 42	Antiproliferative activity against human NCI-H522 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human NCI-H522 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PANC-1	GI₅₀	25.4 μM Compound: 42	Antiproliferative activity against human PANC1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PANC1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
PC-3	GI₅₀	17.1 μM Compound: 42	Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
Raji	GI₅₀	20 μM Compound: 42	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-BR-3	GI₅₀	21 μM Compound: 42	Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-ES1	GI₅₀	7.38 μM Compound: 42	Antiproliferative activity against human SK-ES-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-ES-1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-MEL19	GI₅₀	1.48 μM Compound: 42	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SK-OV-3	GI₅₀	23.5 μM Compound: 42	Antiproliferative activity against human SKOV3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SKOV3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SW480	GI₅₀	8.17 μM Compound: 42	Antiproliferative activity against human SW480 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
SW-620	GI₅₀	8.73 μM Compound: 42	Antiproliferative activity against human SW620 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human SW620 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T47D	GI₅₀	10.8 μM Compound: 42	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
T84	GI₅₀	23.2 μM Compound: 42	Antiproliferative activity against human T84 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human T84 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-251	GI₅₀	17.8 μM Compound: 42	Antiproliferative activity against human U251 cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U251 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]
U-87MG ATCC	GI₅₀	21.7 μM Compound: 42	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	[PMID: 30802730]

体外研究
(In Vitro)

PIM1-IN-1 (Compound 42) 具有抗增殖活性，对黑色素瘤细胞系 SKMEL-19 的 GI₅₀ 为 1.48 μM。PIM1-IN-1与不同的抗肿瘤药物联合在不同的肿瘤细胞系中具有显著的协同作用^[1]。
PIM1-IN-1 (2.5，5，10 μM，24 hours) 诱导 SKMEL19 细胞凋亡^[1]。

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

Apoptosis Analysis^[1]

Cell Line:	SKMEL19 cells
Concentration:	2.5, 5, or 10 µM
Incubation Time:	24 hours
Result:	Regulated cell cycle, induced cell apopsis in SKMEL19 cells.

体内研究
(In Vivo)

PIM1-IN-1 在 BALB-C 小鼠中的清除率为 1.26 L/h/kg^[1]。

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

分子量

474.56

Formula

C₂₅H₃₀N₈O₂

CAS 号

1417630-95-5

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 45 mg/mL (94.82 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	2.1072 mL	10.5361 mL	21.0722 mL
5 mM	0.4214 mL	2.1072 mL	4.2144 mL
10 mM	0.2107 mL	1.0536 mL	2.1072 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, 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。

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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.83%

选择批次：

Data Sheet (606 KB) SDS (251 KB)

COA (286 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Martínez-González S, et al. Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors. Eur J Med Chem. 2019 Feb 19;168:87-109. [Content Brief]

PIM1-IN-1 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	2.1072 mL	10.5361 mL	21.0722 mL	52.6804 mL
	5 mM	0.4214 mL	2.1072 mL	4.2144 mL	10.5361 mL
	10 mM	0.2107 mL	1.0536 mL	2.1072 mL	5.2680 mL
	15 mM	0.1405 mL	0.7024 mL	1.4048 mL	3.5120 mL
	20 mM	0.1054 mL	0.5268 mL	1.0536 mL	2.6340 mL
	25 mM	0.0843 mL	0.4214 mL	0.8429 mL	2.1072 mL
	30 mM	0.0702 mL	0.3512 mL	0.7024 mL	1.7560 mL
	40 mM	0.0527 mL	0.2634 mL	0.5268 mL	1.3170 mL
	50 mM	0.0421 mL	0.2107 mL	0.4214 mL	1.0536 mL
	60 mM	0.0351 mL	0.1756 mL	0.3512 mL	0.8780 mL
	80 mM	0.0263 mL	0.1317 mL	0.2634 mL	0.6585 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:

PIM1-IN-11417630-95-5PimPim kinasesInhibitorinhibitorinhibit

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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。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

PIM1-IN-1

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