Olverembatinib(Synonyms: GZD824; HQP1351)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Olverembatinib (Synonyms: GZD824; HQP1351) 纯度: 99.78%

Olverembatinib (GZD824) 是一种高效的，具有口服活性的 pan-Bcr-Abl 抑制剂。Olverembatinib 能广泛而有效地抑制突变型 Bcr-Abl。Olverembatinib 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 具有抗肿瘤作用。

Olverembatinib(Synonyms: GZD824; HQP1351)

Olverembatinib Chemical Structure

CAS No. : 1257628-77-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1383 In-stock
5 mg ￥1180 In-stock
10 mg ￥2100 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Olverembatinib 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • NMPA-Approved Drug Library
  • Cytoskeleton Compound Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Rare Diseases Drug Library

生物活性

Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib 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 shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].
Olverembatinib selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].
Olverembatinib 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 suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT[1].
Olverembatinib (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 exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].
Olverembatinib 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

532.56

Formula

C29H27F3N6O
CAS 号

1257628-77-5
中文名称

耐克替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (187.77 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 1.8777 mL 9.3886 mL 18.7772 mL
5 mM 0.3755 mL 1.8777 mL 3.7554 mL
10 mM 0.1878 mL 0.9389 mL 1.8777 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: ≥ 2.75 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 27.5 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.16 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 27.5 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务