Olverembatinib dimesylate(Synonyms: GZD824 dimesylate; HQP1351 dimesylate)

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Olverembatinib dimesylate (Synonyms: GZD824 dimesylate; HQP1351 dimesylate) 纯度: 99.81%

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-AblT315I 作用的 IC50 值分别为 0.34 nM 和 0.68 nM。Olverembatinib dimesylate 具有抗肿瘤作用。

Olverembatinib dimesylate(Synonyms: GZD824 dimesylate; HQP1351 dimesylate)

Olverembatinib dimesylate Chemical Structure

CAS No. : 1421783-64-3

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10 mM * 1 mL in DMSO ¥1882 In-stock
5 mg ¥1180 In-stock
10 mg ¥2100 In-stock
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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-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity[1].

IC50 & Target

IC50: 0.68 nM (Bcr-AblT315I), 0.27 nM (Bcr-AblE255K) , 0.71 nM (Bcr-AblG250E) , 0.15 nM (Bcr-AblQ252H), 0.35 nM (Bcr-Abl H396P), 0.29 nM (Bcr-Abl M351T), 0.35 nM (Bcr-AblY253F), Bcr-AblF317L[1]

体外研究
(In Vitro)

Olverembatinib dimesylate shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].
Olverembatinib dimesylate selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].
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-AblT315I(0.1-100 nM; 4.0 hours)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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[1].
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-AblT315I[1].
Olverembatinib dimesylate exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].
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)[1].

上海金畔生物科技有限公司 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-AblT315I[1]
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[1]
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%), Cmax (390.5 μg/L), T1/2 (5.6 h).

Clinical Trial

分子量

724.77

Formula

C31H35F3N6O7S2

CAS 号

1421783-64-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

溶解性数据
In Vitro: 

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3797 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Ren X, Pan X, Zhang Z, Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem. 2013 Feb 14;56(3):879-94.

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