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MGCD265

Cat. No. M1922
MGCD265 Structure
Size Price Availability Quantity
10mg USD 220 In stock
50mg USD 660 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MGCD265 is an orally bioavailable, small molecule tyrosine kinase inhibitor of Met, VEGFR1, VEGFR2, VEGFR3, Ron, and Tie2 with IC50 of 1 nM, 3 nM, 3 nM, 4 nM, 2 nM and 7 nM, respectively. Dysregulation of Met signaling has been implicated in the initiation, progression and metastasis of human cancers. Met is overexpressed in non-small-cell lung cancer and its lack of staining in normal lung tissue makes it an attractive target. Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs. MGCD-265 has demonstrated a favorable safety profile and can be combined safely with other cancer therapeutics such as docetaxel and erlotinib. In preclinical studies, MGCD265 demonstrated nanomolar potency in enzyme and cellular assays and up to 100% of tumor growth inhibition in a broad range of xenograft models. Daily oral administration of MGCD265 was found to be well tolerated at doses of 24, 48 and 96 mg/m2.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 517.6
Formula C26H20FN5O2S2
CAS Number 875337-44-3
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

Targeting the Met pathway in lung cancer.
Belalcazar A, et al. Expert Rev Anticancer Ther. 2012 Apr;12(4):519-28. PMID: 22500688.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MGCD265 supplier, c-Met, inhibitors

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