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XL647

Cat. No. M3780

XL647 Structure

Synonym: EXEL-7647, KD-019

Size Price Availability Quantity
5mg USD 300 In stock
10mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

XL647 is an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression. Check for active clinical trials or closed clinical trials using this agent.Inhibition of EGFR blocks signal transduction and thus impedes vascularization. XL647 inhibits other receptor tyrosine kinases such as Neu (ErbB2), Flk-1 (KDR), EphB4, and Flt-4. XL647 administered on an intermittent or daily-dosing schedule demonstrated antitumor activity in patients with EGFR-activating mutations. The adverse-event profile was similar for the two dosing schedules.

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 491.39
Formula C24H25Cl2FN4O2
CAS Number 781613-23-8 (874286-84-7)
Purity >99%
Solubility DMSO 3 mg/mL
Storage at -20°C
References

Phase II study of the multitargeted tyrosine kinase inhibitor XL647 in patients with non-small-cell lung cancer.
Pietanza MC, et al. J Thorac Oncol. 2012 May;7(5):856-65. PMID: 22722787.

EGFR-mutant lung adenocarcinomas treated first-line with the novel EGFR inhibitor, XL647, can subsequently retain moderate sensitivity to erlotinib.
Chmielecki J, et al. J Thorac Oncol. 2012 Feb;7(2):434-42. PMID: 22173702.

XL647--a multitargeted tyrosine kinase inhibitor: results of a phase II study in subjects with non-small cell lung cancer who have progressed after responding to treatment with either gefitinib or erlotinib.
Pietanza MC, et al. J Thorac Oncol. 2012 Jan;7(1):219-26. PMID: 22011666.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: XL647, EXEL-7647, KD-019 supplier, EGFR/HER2, inhibitors

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