R916562

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R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC₅₀s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.

For research use only. We do not sell to patients.

R916562 Chemical Structure

CAS No. : 1037798-41-6

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Biological Activity
Protocol
Purity & Documentation
References
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Description

R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC₅₀s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis^[1].

IC₅₀ & Target^[1]

Axl

136 nM (IC₅₀)

VEGF-R2

24 nM (IC₅₀)

In Vivo

R916562 treatment at 85 mg/kg or 125 mg/kg orally b.i. d for 21 days results in statistically significant tumor growth inhibitions of 69% or 83% respectively. R916562 shows 73% reduction in fibroblast growth factor-induced neovascularization in a mouse corneal micropocket assay at a dose of 100 mg/kg and 50% reduction at 50 mg/kg^[1].

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

Molecular Weight

536.09

Formula

C₂₆H₃₀ClN₉S

CAS No.

1037798-41-6

SMILES

NC1=NC(NC(C=C2)=CC=C2N3CCN([C@H]4[C@@H]5CC[C@@H](C5)C4)CC3)=NN1C6=NC(Cl)=NC7=C6SC=C7C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Goff D, et al. Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. Bioorg Med Chem Lett. 2017 Aug 15; 27(16):3766-3771. [Content Brief]

Animal Administration ^[1]	Mice^[1] The nu/nu mice are used in the study. In the MDA-MB-231 human breast cancer xenograft model, mice are given 125 mg/kg b.i.d. orally for 21 days. Mean tumor volume is measured^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Goff D, et al. Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. Bioorg Med Chem Lett. 2017 Aug 15; 27(16):3766-3771. [Content Brief]

R916562 Related Classifications

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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:

R9165621037798-41-6R 916562R-916562TAM ReceptorVEGFRTyro3AxlMerVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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