1. Protein Tyrosine Kinase/RTK Apoptosis
  2. PDGFR Bcr-Abl Apoptosis
  3. GZD856 formic

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-AblT315I 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。

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GZD856 formic Chemical Structure

GZD856 formic Chemical Structure

CAS No. : 2804039-78-7

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10 mM * 1 mL in DMSO ¥5090
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1 mg ¥1818
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5 mg ¥4000
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10 mg ¥6800
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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-AblT315I 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]. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1][2]

PDGFRα

68.6 nM (IC50)

PDGFRβ

136.6 nM (IC50)

Bcr-AblT315I

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-AblWT and Bcr-AblT315I, with IC50s of 2.2, 67.0, 0.64 and 10.8 nM, respectively[2].

MCE 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-AblT315I[2].
GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T1/2=19.97 h), optimal plasma exposure (Cmax=934.38 μg/L) and a AUC0-∞ (8165.8 µg/L•h) in rats[1].
GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T1/2=22.2 h), optimal plasma exposure (Cmax=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats[1].

MCE 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.: T1/2=19.97 h; Cmax=934.38 μg/L; AUC0-∞=8165.8 µg/L•h.
P.o.: T1/2=22.2 h; Cmax=899.5 μg/L; BA=78%.
分子量

578.58

Formula

C30H29F3N6O3

CAS 号
性状

固体

颜色

Off-white to light yellow

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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (172.84 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7284 mL 8.6418 mL 17.2837 mL
5 mM 0.3457 mL 1.7284 mL 3.4567 mL
查看完整储备液配制表

* 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)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7284 mL 8.6418 mL 17.2837 mL 43.2092 mL
5 mM 0.3457 mL 1.7284 mL 3.4567 mL 8.6418 mL
10 mM 0.1728 mL 0.8642 mL 1.7284 mL 4.3209 mL
15 mM 0.1152 mL 0.5761 mL 1.1522 mL 2.8806 mL
20 mM 0.0864 mL 0.4321 mL 0.8642 mL 2.1605 mL
25 mM 0.0691 mL 0.3457 mL 0.6913 mL 1.7284 mL
30 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4403 mL
40 mM 0.0432 mL 0.2160 mL 0.4321 mL 1.0802 mL
50 mM 0.0346 mL 0.1728 mL 0.3457 mL 0.8642 mL
60 mM 0.0288 mL 0.1440 mL 0.2881 mL 0.7202 mL
80 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5401 mL
100 mM 0.0173 mL 0.0864 mL 0.1728 mL 0.4321 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
GZD856 formic
目录号:
HY-101489A
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