Olverembatinib dimesylate GZD824 dimesylate; HQP1351 dimesylate|cas:1421783-64-3|西域试剂

Olverembatinib dimesylate GZD824 dimesylate; HQP1351 dimesylate,99.81%

产品编号：Bellancom-15666A| CAS NO：1421783-64-3| 分子式：C₃₁H₃₅F₃N₆O₇S₂| 分子量：724.77

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-15666A		￥1180.00	杭州北京（现货）
Bellancom-15666A		￥2100.00	杭州北京（现货）

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Olverembatinib dimesylate GZD824 dimesylate; HQP1351 dimesylate

产品介绍

Olverembatinib (GZD824) dimesylate 是一种高效的，具有口服活性的 pan-Bcr-Abl 抑制剂。Olverembatinib dimesylate 能广泛而有效地抑制突变型 Bcr-Abl。Olverembatinib dimesylate 对天然的 Bcr-Abl 和 Bcr-Abl^T315I 作用的 IC₅₀ 值分别为 0.34 nM 和 0.68 nM。Olverembatinib dimesylate 具有抗肿瘤作用。

生物活性

Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl^T315I with IC₅₀s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity.

体外研究

Olverembatinib dimesylate shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants.
Olverembatinib dimesylate selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells.
Olverembatinib dimesylate inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-Abl^T315I(0.1-100 nM; 4.0 hours).

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

Western Blot Analysis

Cell Line:	K562 cells
Concentration:	1 nM, 2 nM, 5 nM, 10 nM, 20nM
Incubation Time:	4.0 hours
Result:	Inhibited Bcr-Abl signaling in K562 cell lines.

体内研究
(In Vivo)

Olverembatinib dimesylate suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl ^WT.
Olverembatinib dimesylate (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-Abl^T315I.
Olverembatinib dimesylate exhibits a good oral bioavailability (rat 48.7%) and C_max (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg).
Olverembatinib dimesylate exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg).

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

Animal Model:	SCID nude mice, bearing allografted Ba/F3 cells expressing Bcr-Abl^T315I
Dosage:	1 mg/kg, 2 mg/kg, 5.0 mg/kg, 10 mg/kg, 20 mg/kg
Administration:	Oral gavage, daily, for 10 days
Result:	Efficiently prolonged animal survival in an allograft leukemia tumor model.

Animal Model:	Rats
Dosage:	5 mg/kg for i.v.; 25 mg/kg for oral (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral administration
Result:	Oral bioavailability (48.7%), C_max (390.5 μg/L), T_1/2 (5.6 h).

体内研究

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

Animal Model:	SCID nude mice, bearing allografted Ba/F3 cells expressing Bcr-Abl^T315I
Dosage:	1 mg/kg, 2 mg/kg, 5.0 mg/kg, 10 mg/kg, 20 mg/kg
Administration:	Oral gavage, daily, for 10 days
Result:	Efficiently prolonged animal survival in an allograft leukemia tumor model.

Animal Model:	Rats
Dosage:	5 mg/kg for i.v.; 25 mg/kg for oral (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral administration
Result:	Oral bioavailability (48.7%), C_max (390.5 μg/L), T_1/2 (5.6 h).

体内研究

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

Animal Model:	SCID nude mice, bearing allografted Ba/F3 cells expressing Bcr-Abl^T315I
Dosage:	1 mg/kg, 2 mg/kg, 5.0 mg/kg, 10 mg/kg, 20 mg/kg
Administration:	Oral gavage, daily, for 10 days
Result:	Efficiently prolonged animal survival in an allograft leukemia tumor model.

Animal Model:	Rats
Dosage:	5 mg/kg for i.v.; 25 mg/kg for oral (Pharmacokinetic Analysis)
Administration:	Intravenous injection and oral administration
Result:	Oral bioavailability (48.7%), C_max (390.5 μg/L), T_1/2 (5.6 h).

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (172.47 mM; Need ultrasonic)

H₂O : ≥ 50 mg/mL (68.99 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3797 mL	6.8987 mL	13.7975 mL
5 mM	0.2759 mL	1.3797 mL	2.7595 mL
10 mM	0.1380 mL	0.6899 mL	1.3797 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 and light)。-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 (2.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.87 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 (2.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.87 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 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 (2.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.87 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。