GZD856

发表于2024年10月30日由上海金畔生物科技有限公司

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。

GZD856

GZD856 是一种有效的和具有口服活性的 PDGFRα/β 抑制剂，IC₅₀ 值分别为 68.6 和 136.6 nM。GZD856 也是 Bcr-Abl^T315I 的抑制剂，对天然 Bcr-Abl 和 T315I 突变型的 IC₅₀ 值分别为 19.9 和 15.4 nM。GZD856 具有抗肿瘤活性。

GZD856 Chemical Structure

CAS No. : 1257628-64-0

规格	价格	是否有货
5 mg	￥4000	询问价格 & 货期
10 mg	￥6800	询问价格 & 货期
25 mg	￥13500	询问价格 & 货期
50 mg	￥22000	询问价格 & 货期
100 mg	￥34000	询问价格 & 货期

* Please select Quantity before adding items.

GZD856 的其他形式现货产品:

GZD856 formic

生物活性

GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC₅₀s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl^T315I inhibitor, with IC₅₀s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity^[1]^[2].

IC₅₀ & Target^[1]^[2]

PDGFRα

68.6 nM (IC₅₀)

PDGFRβ

136.6 nM (IC₅₀)

Bcr-Abl^T315I

15.4 nM (IC₅₀)

Bcr-Abl

19.9 nM (IC₅₀)

体外研究
(In Vitro)

GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells^[1].
GZD856 (0.3-3 μM; 24-28 h) induces a dose-dependent G0/G1 phase arrest and apoptosis in H1703 but not A549 cells^[1].
GZD856 (0.1-10 μM; 6 h) dose-dependently inhibits the PDGFRα/β phosphorylation and downstream signaling in H1703 and A549 cells^[1].
GZD856 inhibits the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-Abl^WT and Bcr-Abl^T315I, with IC₅₀s of 2.2, 67.0, 0.64 and 10.8 nM, respectively^[2].

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.

Cell Viability Assay^[1]

Cell Line:	H1703, A549, Calu-6, 95-D, L-78, HCC827, SPCA-1, H1650, H1299, H522, H332 and H820 NSCLC cells
Concentration:	0.0032-10 μM
Incubation Time:	72 hours
Result:	Inhibited PDGFRα-overexpressing H1703 cells, with an IC₅₀ of 0.25 μM.

Apoptosis Analysis^[1]

Cell Line:	H1703 and A549 NSCLC cells
Concentration:	0.3, 1, 3 μM
Incubation Time:	24, 48 hours
Result:	Led to 54.1% apoptosis in H1703 cells at the concentration of 3.0 µM, whereas only 15.5% apoptotic A549 cells were observed under similar conditions. Decreased the CDK4, cyclin D2, CDK2 and Cyclin E protein levels and activated of PARP and Caspase-3 cleavage in H1703 cells.

Western Blot Analysis^[1]

Cell Line:	H1703 and A549 NSCLC cells
Concentration:	0.1-10 μM
Incubation Time:	6 hours
Result:	Inhibited the phosphorylation of PDGFRα and PDGFRβ in a dose-dependent manner. Observed the activation of downstream AKT, ERK1/2 and STAT3, with no obvious effects on total protein levels.

体内研究
(In Vivo)

GZD856 (10-30 mg/kg, p.o. once daily for 16 d) displays good antitumor activity in both H1703 and A549 lung cancer models and is well tolerated. GZD856 inhibits brain and liver metastasis of lung cancer cells in an A549-Luc orthotopic model^[1].
GZD856 (10 mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-Abl^T315I^[2].
GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T_1/2=19.97 h), optimal plasma exposure (C_max=934.38 μg/L) and a AUC_0-∞ (8165.8 µg/L•h) in rats^[1].
GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T_1/2=22.2 h), optimal plasma exposure (C_max=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats^[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:	Male CB17-SCID mice implanted with H1703 and A549 cancer cells^[1]
Dosage:	10, 30 mg/kg
Administration:	Oral gavage once daily for 16 days
Result:	Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively. Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg. Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight.

Animal Model:	Sprague-Dawley (SD) rats (180-220 g)^[1]
Dosage:	5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:	A single intravenous injection and oral administration
Result:	I.v.: T_1/2=19.97 h; C_max=934.38 μg/L; AUC_0-∞=8165.8 µg/L•h. P.o.: T_1/2=22.2 h; C_max=899.5 μg/L; BA=78%.

分子量

532.56

Formula

C₂₉H₂₇F₃N₆O

CAS 号

1257628-64-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : 250 mg/mL (469.43 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8777 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

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 (3.91 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.91 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 (3.91 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.91 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

*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]. Zhang Z, et al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178.

[2]. Lu X, et al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32(1):331-336.

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

Olverembatinib(Synonyms: GZD824; HQP1351)

发表于2024年4月28日由上海金畔生物科技有限公司

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-Abl^T315I 作用的 IC₅₀ 值分别为 0.34 nM 和 0.68 nM。Olverembatinib 具有抗肿瘤作用。

Olverembatinib Chemical Structure

CAS No. : 1257628-77-5

规格	价格	是否有货
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-Abl^T315I with IC₅₀s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity^[1].

IC₅₀ & Target

IC50: 0.68 nM (Bcr-Abl^T315I), 0.27 nM (Bcr-Abl^E255K) , 0.71 nM (Bcr-Abl^G250E) , 0.15 nM (Bcr-Abl^Q252H), 0.35 nM (Bcr-Abl^H396P), 0.29 nM (Bcr-Abl^M351T), 0.35 nM (Bcr-Abl^Y253F), Bcr-Abl^F317L^[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-Abl^T315I(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-Abl^T315I^[1].
Olverembatinib exhibits a good oral bioavailability (rat 48.7%) and C_max (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-Abl^T315I^[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%), C_max (390.5 μg/L), T_1/2 (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：

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

GZD856 formic

发表于2024年2月23日由上海金畔生物科技有限公司

GZD856 formic 纯度: 98.06%

GZD856 formic 是一种有效的和具有口服活性的 PDGFRα/β 抑制剂，IC₅₀ 值分别为 68.6 和 136.6 nM。GZD856 formic 也是 Bcr-Abl^T315I 的抑制剂，对天然 Bcr-Abl 和 T315I 突变型的 IC₅₀ 值分别为 19.9 和 15.4 nM。GZD856 formic 具有抗肿瘤活性。

GZD856 formic Chemical Structure

规格	价格	是否有货
5 mg	￥4000	In-stock
10 mg	￥6800	In-stock
25 mg	￥13500	In-stock
50 mg	￥22000	In-stock
100 mg	￥34000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

GZD856 formic 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Cytoskeleton Compound Library
Orally Active Compound Library
Anti-Alzheimer’s Disease Compound Library
Anti-Lung Cancer Compound Library
Anti-Blood Cancer Compound Library
Anti-Parkinson’s Disease Compound Library
Neurodegenerative Disease-related Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library

生物活性

IC₅₀ & Target^[1]^[2]

PDGFRα

68.6 nM (IC₅₀)

PDGFRβ

136.6 nM (IC₅₀)

Bcr-Abl^T315I

15.4 nM (IC₅₀)

Bcr-Abl

19.9 nM (IC₅₀)

体外研究
(In Vitro)

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.

Cell Viability Assay^[1]

Cell Line:	H1703, A549, Calu-6, 95-D, L-78, HCC827, SPCA-1, H1650, H1299, H522, H332 and H820 NSCLC cells
Concentration:	0.0032-10 μM
Incubation Time:	72 hours
Result:	Inhibited PDGFRα-overexpressing H1703 cells, with an IC₅₀ of 0.25 μM.

Apoptosis Analysis^[1]

Cell Line:	H1703 and A549 NSCLC cells
Concentration:	0.3, 1, 3 μM
Incubation Time:	24, 48 hours
Result:	Led to 54.1% apoptosis in H1703 cells at the concentration of 3.0 µM, whereas only 15.5% apoptotic A549 cells were observed under similar conditions. Decreased the CDK4, cyclin D2, CDK2 and Cyclin E protein levels and activated of PARP and Caspase-3 cleavage in H1703 cells.

Western Blot Analysis^[1]

Cell Line:	H1703 and A549 NSCLC cells
Concentration:	0.1-10 μM
Incubation Time:	6 hours
Result:	Inhibited the phosphorylation of PDGFRα and PDGFRβ in a dose-dependent manner. Observed the activation of downstream AKT, ERK1/2 and STAT3, with no obvious effects on total protein levels.

体内研究
(In Vivo)

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:	Male CB17-SCID mice implanted with H1703 and A549 cancer cells^[1]
Dosage:	10, 30 mg/kg
Administration:	Oral gavage once daily for 16 days
Result:	Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively. Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg. Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight.

Animal Model:	Sprague-Dawley (SD) rats (180-220 g)^[1]
Dosage:	5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:	A single intravenous injection and oral administration
Result:	I.v.: T_1/2=19.97 h; C_max=934.38 μg/L; AUC_0-∞=8165.8 µg/L•h. P.o.: T_1/2=22.2 h; C_max=899.5 μg/L; BA=78%.

分子量

578.58

Formula

C₃₀H₂₉F₃N₆O₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

参考文献

[1]. Zhang Z, et, al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178.

[2]. Lu X, et, al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl T315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32(1):331-336.

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

whatman (沃特曼)

英国沃特曼 Millipore PALL中国代理商金畔官网

标签归档：gzd

GZD856

Olverembatinib(Synonyms: GZD824; HQP1351)

Olverembatinib 相关产品

•相关化合物库:

GZD856 formic

GZD856 formic 相关产品

•相关化合物库:

2024年 11月
一	二	三	四	五	六	日
				1	2	3
4	5	6	7	8	9	10
11	12	13	14	15	16	17
18	19	20	21	22	23	24
25	26	27	28	29	30