KRCA-0008|cas:1472795-20-2|西域试剂

KRCA-0008,98.88%

产品编号：Bellancom-12331| CAS NO：1472795-20-2| 分子式：C₃₀H₃₇ClN₈O₄| 分子量：609.12

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12331	￥650.00	杭州北京（现货）
Bellancom-12331	￥1100.00	杭州北京（现货）
Bellancom-12331	￥1980.00	杭州北京（现货）
Bellancom-12331	￥3880.00	杭州北京（现货）
Bellancom-12331	￥6600.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

KRCA-0008

产品介绍

KRCA-0008 是选择性的 ALK/Ack1 抑制剂，对 ALK 和 Ack1 的 IC₅₀ 值分别为 12 和 4 nM。KRCA-0008 可用于癌症的研究。

生物活性

KRCA-0008 is a selective ALK/Ack1 inhibitor with IC₅₀s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer.

体外研究

KRCA-0008 (0-1000 μM) shows potency to ALK (wt), ALK L1196 M, ALK C1156Y, ALK F1174L, ALK R1275Q and insulin receptor with IC₅₀s of 12, 75, 4, 17, 17 and 210 nM, respectively.
KRCA-0008 (0-1000 nM; 4 h) inhibits ALK-dependent signaling pathways more potently than crizotinib.
KRCA-0008 (0-1000 nM; 72 h) induces cell apoptosis.
KRCA-0008 (0-100 nM; 48 h) affects cell cycle.

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

Cell Proliferation Assay

Cell Line:	H3122 and H1993 cell lines
Concentration:	200 nM
Incubation Time:	6 hours
Result:	Inhibited cell proliferation of H3122 and H1993 cells with IC₅₀s of 0.08 and 3.6 nM, respectively.

Cell Proliferation Assay

Cell Line:	NPM-ALK-positive ALCL cell lines (Karpas-299 and SU-DHL-1) and U937 NPM ALK-negative lymphoma cell line
Concentration:	200 nM
Incubation Time:	72 hours
Result:	Inhibited proliferation of Karpas-299, SU-DHL-1 and U937 cells with GI₅₀s of 12 nM, 3 nM and 3.5 μM, respectively.

Western Blot Analysis

Cell Line:	Karpas-299 and SU-DHL-1 cell lines
Concentration:	0, 10, 100 and 1000 nM
Incubation Time:	4 hours
Result:	Completely suppressed phosphorylation of ALK and its effectors at a dose of 100 nM in NPM-ALK-positive ALCL cells.

Apoptosis Analysis

Cell Line:	SU-DHL-1 cell line
Concentration:	0-1 μM
Incubation Time:	72 hours
Result:	Dose-dependently increased cspase-3/7 activities and induced cell apoptosis.

Cell Cycle Analysis

Cell Line:	Karpas-299 and SU-DHL-1 cell lines
Concentration:	0-100 nM
Incubation Time:	48 hours
Result:	Induced G0/G1 cell cycle arrest in ALCL cells expressing NPM-ALK.

体内研究
(In Vivo)

KRCA-0008 (25 and 50 mg/kg; p.o. twice a day for two weeks) suppresses tumor growth in an ALK-positive Karpas-299 xenograft model.

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

Animal Model:	NOD/SCID mice with Karpas-299 xenografts
Dosage:	25 and 50 mg/kg
Administration:	Oral gavage; 25 and 50 mg/kg twice a day; for two weeks
Result:	Significantly inhibited tumor growth by inhibiting NPM-ALK phosphorylation without showing overt signs of toxicity or significant compound-related body weight loss.

体内研究

KRCA-0008 (25 and 50 mg/kg; p.o. twice a day for two weeks) suppresses tumor growth in an ALK-positive Karpas-299 xenograft model.

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

Animal Model:	NOD/SCID mice with Karpas-299 xenografts
Dosage:	25 and 50 mg/kg
Administration:	Oral gavage; 25 and 50 mg/kg twice a day; for two weeks
Result:	Significantly inhibited tumor growth by inhibiting NPM-ALK phosphorylation without showing overt signs of toxicity or significant compound-related body weight loss.

体内研究

KRCA-0008 (25 and 50 mg/kg; p.o. twice a day for two weeks) suppresses tumor growth in an ALK-positive Karpas-299 xenograft model.

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

Animal Model:	NOD/SCID mice with Karpas-299 xenografts
Dosage:	25 and 50 mg/kg
Administration:	Oral gavage; 25 and 50 mg/kg twice a day; for two weeks
Result:	Significantly inhibited tumor growth by inhibiting NPM-ALK phosphorylation without showing overt signs of toxicity or significant compound-related body weight loss.

性状

Solid

溶解性数据

In Vitro:

DMSO : 230 mg/mL (377.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6417 mL	8.2086 mL	16.4171 mL
5 mM	0.3283 mL	1.6417 mL	3.2834 mL
10 mM	0.1642 mL	0.8209 mL	1.6417 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution

此方案可获得 ≥ 5.75 mg/mL (9.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 57.5 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。
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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution

此方案可获得 ≥ 5.75 mg/mL (9.44 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 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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