AMG458

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Cat No.

CEI-0032

Description

AMG458

CAS_No

913376-83-7

Molecular Weight

539.58

Purity

>99%

Storage

2 years at -20 centigrade

Targets

human c-Met

Molecular Formula

C30H29N5O5

Solubility

In vitro

AMG 458 can potently inhibit human c-Met and mouse c-Met with Ki of 1.2 nM or 2.0 nM. AMG-458 enhances radiosensitivity in H441 but not in A549. A549 expresses low levels of c-Met, which were phosphorylated only in the presence of exogenous hepatocyte growth factor. The combination of radiation therapy and AMG-458 treatment synergistically increase apoptosis in the H441 cell line but not in A549. Radiation therapy, AMG-458, and combination treatment were found to reduce p-Akt and p-Erk levels in H441 but not in A549. H441 became less sensitive to AMG-458 after small interfering RNA knockdown of c-Met; there was no change in A549. After overexpression of c-Met, A549 became more sensitive, while H441 became less sensitive to AMG-458. AMG-458 is more effective in cells that expressed higher levels of c-Met/p-Met.

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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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