2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. AMG-458

AMG-458 是有效的、选择性的、具有口服活性的 c-Met 抑制剂，其对人和小鼠的 Ki 值分别为 1.2 nM 和 2.0 nM。

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AMG-458 Chemical Structure

AMG-458 Chemical Structure

CAS No. : 913376-83-7

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1465
In-stock
1 mg ￥429
In-stock
5 mg ￥1234
In-stock
10 mg ￥1925
In-stock
25 mg ￥3238
In-stock
50 mg ￥4625
In-stock
100 mg 现货 询价
500 mg 现货 询价
1 g   询价  
5 g   询价  

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Customer Review

AMG-458 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

AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively[1].

IC50 & Target[1]

VEGDR2

4100 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
NIH3T3 ED50
12 mg/kg
Compound: 17
Antitumor activity in TPR-Met expressing human NIH3T3 cells xenografted in po dosed mouse assessed as tumor growth inhibition after 24 hrs
Antitumor activity in TPR-Met expressing human NIH3T3 cells xenografted in po dosed mouse assessed as tumor growth inhibition after 24 hrs
[PMID: 18553959]
PC-3 IC50
60.1 nM
Compound: 59e, AMG-458
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
[PMID: 22320327]
U-87MG ATCC ED50
16 mg/kg
Compound: 17
Antitumor activity in human U87MG cells xenografted orally dosed CD1 NU/NU mouse assessed as tumor growth inhibition after 14 days
Antitumor activity in human U87MG cells xenografted orally dosed CD1 NU/NU mouse assessed as tumor growth inhibition after 14 days
[PMID: 18553959]
体内研究
(In Vivo)

AMG-458 (orally, 30, 100 mg/kg) significantly inhibits tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight[1].

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

Animal Model: NIH-3T3/TPR-Met model and U-87 MG human glioblastoma xenograft model[1].
Dosage: 10, 30, 100 mg/kg.
Administration: Orally q.d. or b.i.d.
Result: With an ED50 of ∼12 mg/kg and an ED90 of ∼ 34 mg/kg in NIH-3T3/TPR-Met model.
With an ED50 of ∼16 mg/kg and an ED90 of ∼ 59 mg/kg in U-87 MG human glioblastoma xenograft model.
Significantly inhibited tumor growth at 30 and 100 mg/kg q.d. and 30 mg/kg b.i.d. without adverse effect on body weight.
Animal Model: Balb/c mouse and SD rat[1].
Dosage: 1 mg/kg (Pharmacokinetic Analysis).
Administration: IV dose: 1 mg/kg (20% Captisol with pH adjusted to 3.5 using methanesulfonic acid).
Result: Exhibited CL ((L/h)/kg) values of 0.16 and 0.73, Vss (L/kg) values of 0.31 and 0.62, t1/2 (h) values of 1.3 and 1.0 in mouse and rat, respectively.
分子量

539.58

Formula

C30H29N5O5
CAS 号
性状

固体

颜色

Off-white to pink

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
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (92.66 mM; 超声助溶 (<60°C); 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 1.8533 mL 9.2665 mL 18.5329 mL
5 mM 0.3707 mL 1.8533 mL 3.7066 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。-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

AMG-458 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。-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 1.8533 mL 9.2665 mL 18.5329 mL 46.3323 mL
5 mM 0.3707 mL 1.8533 mL 3.7066 mL 9.2665 mL
10 mM 0.1853 mL 0.9266 mL 1.8533 mL 4.6332 mL
15 mM 0.1236 mL 0.6178 mL 1.2355 mL 3.0888 mL
20 mM 0.0927 mL 0.4633 mL 0.9266 mL 2.3166 mL
25 mM 0.0741 mL 0.3707 mL 0.7413 mL 1.8533 mL
30 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
40 mM 0.0463 mL 0.2317 mL 0.4633 mL 1.1583 mL
50 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9266 mL
60 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
80 mM 0.0232 mL 0.1158 mL 0.2317 mL 0.5792 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:

AMG-458913376-83-7AMG458AMG 458c-Met/HGFRInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-14723
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