DBPR112|cas:1226549-49-0|西域试剂

DBPR112,98.07%

产品编号：Bellancom-128778| CAS NO：1226549-49-0| 分子式：C₃₂H₃₁N₅O₃| 分子量：533.62

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货号	价格	库存与货期
Bellancom-128778	￥4500.00	杭州北京（现货）
Bellancom-128778	￥8000.00	杭州北京（现货）
Bellancom-128778	￥16500.00	杭州北京（现货）
Bellancom-128778	￥25500.00	杭州北京（现货）
Bellancom-128778	￥38000.00	杭州北京（现货）

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DBPR112

产品介绍

DBPR112 是一种口服有效的基于氟嘧啶的 EGFR 抑制剂，对 EGFR^WT 和 EGFR^L858R/T790M 的 IC₅₀ 分别为 15 nM 和 48 nM。DBPR112 可以占据 ATP 结合位点。DBPR112 具有显着的抗肿瘤功效。

生物活性

DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC₅₀s of 15 nM and 48 nM for EGFR^WT and EGFR^L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.

体外研究

DBPR112 (compound 78; 0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner.
DBPR112 shows the inhibitory activity against HCC827 (CC₅₀=25 nM), H1975 (CC₅₀=620 nM) and A431 Cell (CC₅₀=1.02 μM) cell lines.
DBPR112 occupies the ATP-binding site and interacts with surrounding residues by covalent bonding, hydrogen bonds, and hydrophobic interactions, which give it a potent inhibitory activity against WT EGFR.

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

Western Blot Analysis

Cell Line:	H1975 cells
Concentration:	0.32, 1.6, 8.0, 40, 200, 1000 nM
Incubation Time:	16 hours
Result:	Induced reduction of phosphorylated EGFR in a dose-dependent manner in H1975 cells.

体内研究
(In Vivo)

DBPR112 (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. DBPR112 (orally; 50 mg/kg; once a day for 15 days) has a significant antitumor effect (mean tumor growth inhibition of 34%) in H1975 tumor model.
DBPR112 (IV; 5 mg/kg) has a T_1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V_ss of 8.6 L/kg for rats.

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

Animal Model:	HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)
Dosage:	20, 50 mg/kg
Administration:	Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
Result:	Significantly reduced tumor growth.

Animal Model:	Rats
Dosage:	5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V_ss of 8.6 L/kg by IV. Had a T_1/2 of 3.4 hours, a C_max of 508 ng/mL and an AUC of 2978 ng/mL•h by PO.

体内研究

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

Animal Model:	HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)
Dosage:	20, 50 mg/kg
Administration:	Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
Result:	Significantly reduced tumor growth.

Animal Model:	Rats
Dosage:	5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V_ss of 8.6 L/kg by IV. Had a T_1/2 of 3.4 hours, a C_max of 508 ng/mL and an AUC of 2978 ng/mL•h by PO.

体内研究

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

Animal Model:	HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)
Dosage:	20, 50 mg/kg
Administration:	Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
Result:	Significantly reduced tumor growth.

Animal Model:	Rats
Dosage:	5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V_ss of 8.6 L/kg by IV. Had a T_1/2 of 3.4 hours, a C_max of 508 ng/mL and an AUC of 2978 ng/mL•h by PO.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (468.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8740 mL	9.3700 mL	18.7399 mL
5 mM	0.3748 mL	1.8740 mL	3.7480 mL
10 mM	0.1874 mL	0.9370 mL	1.8740 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: ≥ 2.08 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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-CD in saline)
Solubility: 2.08 mg/mL (3.90 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.90 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 20.8 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.90 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。