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XL647

Cat. No. M3780
XL647 Structure
Synonym:

EXEL-7647, KD-019

Size Price Availability
5mg USD 300  USD300 Custom Synthesis
10mg USD 550  USD550 Custom Synthesis
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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.

Chemical Information
Molecular Weight 491.39
Formula C24H25Cl2FN4O2
CAS Number 781613-23-8 (874286-84-7)
Solubility (25°C) DMSO 3 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Pietanza MC, et al. J Thorac Oncol. Phase II study of the multitargeted tyrosine kinase inhibitor XL647 in patients with non-small-cell lung cancer.

[2] Chmielecki J, et al. J Thorac Oncol. EGFR-mutant lung adenocarcinomas treated first-line with the novel EGFR inhibitor, XL647, can subsequently retain moderate sensitivity to erlotinib.

[3] Pietanza MC, et al. J Thorac Oncol. 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.

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

 
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