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  4. SPH5030

SPH5030 是选择性的，不可逆的 HER2 抑制剂。SPH5030 抑制 HER2WT 以及 EGFRWT，其 IC50 值分别为 3.51 和 8.13 nM。SPH5030 可用于癌症的研究。

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SPH5030 Chemical Structure

SPH5030 Chemical Structure

CAS No. : 2364326-23-6

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规格 价格 是否有货 数量
1 mg ￥3400
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Customer Review

SPH5030 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer[1].

IC50 & Target

IC50: 3.51 nM (HER2WT), 0.42 nM (HER2D769H), 0.43 nM (HER2D769Y), 0.16 nM (HER2V777L), 0.56 nM (HER2R896C), 8.13 nM (EGFRWT)[1]
体外研究
(In Vitro)

SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines[1].

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

SPH5030 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: NCI-N87, BT-474, SK-BR-3 with HER2 overexpression, MDA-MB-468 with EGFR overexpression, NCI-H441, Es-2, MFE-280, NUGC-4, COLO678, KM12-luc and BaF3 cell lines
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Effectively inhibited NCI-N87, BT-474, SK-BR-3 with HER2 overexpression and BaF3 cells with IC50s of 1.09, 2.01, 20.09 and 6.3 nM, respectively. Poorly inhibited MDA-MB-468 with EGFR overexpression, NCI-H441, Es-2, MFE-280, NUGC-4, COLO678 and KM12-luc cells with IC50s of 2980, 4257, 2716, 3967, 1218, 6065 and 3597 nM, respectively.
体内研究
(In Vivo)

SPH5030 (5-40 mg/kg; p.o. once per day for 13 or 21 days) shows in vivo antitumor efficacy in mice with xenograft tumor models[1].
1.19 Pharmacokinetic Properties of SPH5030 in Mice and Rats[1].

Mice
IV 3 mg/kg		 Mice
PO 10 mg/kg		 Rats
IV 3 mg/kg		 Rats
PO 6 mg/kg
CL (L/kg·h) 0.70±0.20 0.78±0.13
t1/2 (h) 3.76±0.15 3.60±0.59 4.56±0.20 4.38±0.35
Vss (L/kg) 2.96±0.96 3.55±0.64
Cmax (μg/mL) 1.90±0.14 0.76±0.33
tmax (h) 2.67±1.15 3.33±1.15
AUC0-t (h·μg/mL) 13.07±0.48 5.47±2.82
F (%) 87.66 71.35

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

Animal Model: BALB/c nude mouse with NCI-N87 and BT474 xenografts, and NPSG mouse with BAF3 HER2 A775_G776insYVMA xenografts[1]
Dosage: 5, 10, 20 and 40 mg/kg
Administration: Oral gavage; 5-40 mg/kg once per day; for 13 or 21 days
Result: Dose-dependently inhibited tumor growth in NCI-N87, BT474 and BAF3 HER2 A775_G776insYVMA xenograft mouse models, and showed an equivalent or better activity of tumor inhibition compared with neratinib and pyrotinib at a dose of 20 mg/kg. Showed no mortality or significant loss of body weight in xenograft mouse models.
Clinical Trial
分子量

582.63

Formula

C31H31FN8O3
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

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (171.64 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" 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 1.7164 mL 8.5818 mL 17.1636 mL
5 mM 0.3433 mL 1.7164 mL 3.4327 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 (protect from light, stored under nitrogen)。-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

只
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

SPH5030 相关分类

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 (protect from light, stored under nitrogen)。-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 1.7164 mL 8.5818 mL 17.1636 mL 42.9089 mL
5 mM 0.3433 mL 1.7164 mL 3.4327 mL 8.5818 mL
10 mM 0.1716 mL 0.8582 mL 1.7164 mL 4.2909 mL
15 mM 0.1144 mL 0.5721 mL 1.1442 mL 2.8606 mL
20 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1454 mL
25 mM 0.0687 mL 0.3433 mL 0.6865 mL 1.7164 mL
30 mM 0.0572 mL 0.2861 mL 0.5721 mL 1.4303 mL
40 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0727 mL
50 mM 0.0343 mL 0.1716 mL 0.3433 mL 0.8582 mL
60 mM 0.0286 mL 0.1430 mL 0.2861 mL 0.7151 mL
80 mM 0.0215 mL 0.1073 mL 0.2145 mL 0.5364 mL
100 mM 0.0172 mL 0.0858 mL 0.1716 mL 0.4291 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.

Keywords:

SPH50302364326-23-6SPH 5030SPH-5030OthersNCI-N87irreversibleanti-tumormutantneratinibpyrotinibInhibitorinhibitorinhibit

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