JAK3-IN-1 - CAS:1805787-93-2

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JAK3-IN-1

目录号 : KM11949 CAS No. : 1805787-93-2 纯度 : 98%

Data Sheet 产品使用指南

JAK3-IN-1 是一种有效，选择性和口服活性的 JAK3 抑制剂，IC₅₀ 为 4.8 nM。与 JAK1 (IC₅₀ 为 896 nM) 和 JAK 2 (IC₅₀ 为 1050 nM) 相比，JAK3-IN-1 对 JAK3 的选择性高 180 倍以上。

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生物活性

JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC₅₀ of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC₅₀ of 896 nM) and JAK2 (IC₅₀ of 1050 nM).

体外研究

JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM.
. JAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC₅₀ = 13 nM), TTK protein kinase (TTK, IC₅₀ = 49 nM), BLK proto-oncogene (BLK, IC₅₀ = 157 nM) and tyrosine protein kinase TXK (TXK, IC₅₀ = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC₅₀s against EGFRWT and TYK2 (IC₅₀s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC₅₀s for BTK or ITK (IC₅₀s = 794 and 1070 nM respectively).
JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC₅₀ = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM.

Western Blot Analysis

Cell Line:	BMDMs cells
Concentration:	0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM
Incubation Time:	3 hours
Result:	Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 μM.

体内研究

JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T_1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%. After oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced.

分子式

C₂₆H₃₀ClN₇O₂

分子量

508.02

CAS号

1805787-93-2

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

In Vitro:

DMSO : 100 mg/mL (196.84 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9684 mL	9.8421 mL	19.6843 mL
5 mM	0.3937 mL	1.9684 mL	3.9369 mL
10 mM	0.1968 mL	0.9842 mL	1.9684 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.92 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.92 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.92 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。

纯度： 98%

Data Sheet

产品使用指南

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