CRT0066101 (hydrochloride) - CAS:1781742-22-0

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CRT0066101 (hydrochloride) (Synonyms:CRT0066101 trihydrochloride)

目录号 : KCM12033 CAS No. : 1781742-22-0 纯度 : ≥95%

Data Sheet 产品使用指南

Protein kinase D (PKD) is a serine/threonine protein kinase that is activated by diacylglycerol, commonly downstream of PKC signaling. The three human PKD isoforms target a variety of proteins to alter cell proliferation, survival, invasion, and protein transport. CRT0066101 is an inhibitor of all three PKD isoforms (ICs = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively). It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. It can block cell proliferation, induce apoptosis, and reduce the viability of pancreatic cancer cells both in vitro and in vivo.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

CRT0066101 (hydrochloride) is the trihydrochloride salt form of CRT0066101. CRT0066101 (hydrochloride) is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 (hydrochloride) is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 (hydrochloride) exhibits anti-inflammatory activity in mice LPS induced lung injury models, and has anticancer effects.

体外研究

CRT0066101 trihydrochloride (5 µM; 1 h) can block basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 eliminates NT-induced Hsp27 (pS82-Hsp27) phosphorylation, attenuates PKD1-mediated NF-κB activation, and abolishes the expression of NF-κB-dependent proliferative and pro-survival proteins.
CRT0066101 trihydrochloride significantly inhibits the proliferation of Panc-1 cells, with an IC₅₀ value of 1 µM. It induces apoptosis in Panc-1 cells 6-10-fold. CRT0066101 markedly reduces the proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but has some effect on Capan-2 cells.

Western Blot Analysis

Cell Line:	Panc-1 and Panc-28 cells stimulation with neurotensin (NT)
Concentration:	5 µM
Incubation Time:	1 hour
Result:	Blocked both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2).

体内研究

CRT0066101 trihydrochloride (80 mg/kg/day; oral gavage; once daily; for 21 days) effectively inhibits tumor growth in vivo in the Panc-1 orthotopic model. CRT0066101 trihydrochloride (10 mg/kg, intraperitoneal injection, every other day for three doses) provides protective effects against LPS-induced pneumonia in C57BL/6J mice and mitigates lung injury.

Animal Model:	CR-UK nu/nu mice injected with Panc-1 cells
Dosage:	80 mg/kg/day
Administration:	Oral gavage; once daily; for 21 days
Result:	Potently blocked tumor growth in vivo.

Animal Model:	LPS induced lung injury in C57BL/6J mice
Dosage:	10 mg/kg
Administration:	i.p., once every two days for 3 times
Result:	Inhibited the expression of MyD88 and TLR4, inhibited the phosphorylation of NF-κB, ERK and JNK.

分子式

C₁₈H₂₂N₆O^.₃HCl

分子量

447.79

CAS号

1781742-22-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 20 mg/mL (44.66 mM; warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2332 mL	11.1659 mL	22.3319 mL
5 mM	0.4466 mL	2.2332 mL	4.4664 mL
10 mM	0.2233 mL	1.1166 mL	2.2332 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 (sealed storage, away from moisture)。-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 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.47 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。