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Ceritinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ceritinib图片
CAS NO:1032900-25-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议
2 g电议
5 g电议
10 g电议
50 g电议

产品名称
色瑞替尼
LDK378
产品介绍
Ceritinib (LDK378) 是一种选择性,具有口服活性的且具有 ATP 竞争性的ALK酪氨酸激酶抑制剂,IC50为 200 pM。 Ceritinib (LDK378) 还抑制IGF-1RInsRSTK22DIC50值分别为 8、7 和 23 nM。Ceritinib (LDK378) 显示出良好抗肿瘤效力。
生物活性

Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitiveALKtyrosine kinase inhibitor with anIC50of 200 pM. Ceritinib (LDK378) also inhibitsIGF-1R,InsR, andSTK22DwithIC50values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency[1][2].

IC50& Target

IC50: 0.2 nM (ALK), 7 nM (InsR), 8 nM (IGF-1R), 23 nM (STK22D), 60 nM (FLT3), 260 nM (FGFR2)[1]

体外研究
(In Vitro)

Ceritinib (LDK378) also inhibits RET (IC50=400 nM), FGFR3 (IC50=430 nM), LCK (IC50=560 nM), JAK2 (IC50=610 nM), Aurora (IC50=660 nM), LYN (50=840 nM), EGFR (IC50=900 nM), and FGFR4 (IC50=950 nM)[1]. Ceritinib (LDK378) retains high potency against the ALK enzymatic activity with an IC50value of 200 pM and shows only strong inhibition against IGF-1R, InsR, and STK22D out of a panel of 46 kinases with a minimum selectivity of 70-fold. In Ba/F3 cells transfected with various kinases, Ceritinib inhibits ALK activity with an IC50value of 40.7 nM and had IC50values of >100 nM against all other kinases tested. Ceritinib (LDK378) shows potent antiproliferative activity with an IC50value of 22.8 nM in Karpas 299 human non-Hodgkin’s Ki-positive large cell lymphoma carrying the NPM-ALK fusion gene and 26 nM in Ba/F3 cells transfected with the NPM-ALK fusion gene. Ceritinib also shows good selectivity over wild-type Ba/F3 cells (IC50>2 μM) and Ba/F3 cells transfected with Tel-InsR gene (IC50=320 nM)[2].

体内研究
(In Vivo)

Ceritinib (LDK378) has an excellent pharmacokinetics profile in rodents and non-rodents with an oral bioavailability of >50%. Ceritinib demonstrates dose-dependent tumor growth inhibition and achieved partial tumor regression in the Karpas 299 rat xenograft model with daily administration but is capable of achieving complete tumor regression in the H2228 NSCLC rat xenograft model, which carries the EML4-ALK fusion gene. In both models, Ceritinib (LDK378) is well tolerated in animals. Ceritinib (LDK378) is further assessed for its ADME profile and is found to have a relatively good metabolic stability in liver microsomes, modest CYP3A4 inhibition, some hERG inhibition with an IC50value of 46 μM in hERG patch clamp experiments, but no evidence of QTc prolongation in both dog and monkey telemetry studies[2].

Clinical Trial
分子量

558.14

性状

Solid

Formula

C28H36ClN5O3S

CAS 号

1032900-25-6

中文名称

色瑞替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL(22.40 mM;ultrasonic and warming and heat to 60℃)

Ethanol : ≥ 3.33 mg/mL(5.97 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7917 mL8.9583 mL17.9167 mL
5 mM0.3583 mL1.7917 mL3.5833 mL
10 mM0.1792 mL0.8958 mL1.7917 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ≥ 0.5 mg/mL (0.90 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.5 mg/mL (0.90 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 0.5 mg/mL (0.90 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (0.90 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 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。