You have no items in your shopping cart.
|Storage||at -20°C 2 years|
|Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.|
|Solubility (25°C) *||In vitro||DMSO||97 mg/mL (200.9 mM)|
|Water||<1 mg/mL (<1 mM)|
|Ethanol||<1 mg/mL (<1 mM)|
|In vivo||30% PEG400/0.5% Tween80/5% propylene glycol||30 mg/mL|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Regorafenib (also known as BAY 73-4506) is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. It is currently being studied as a potential treatment option in multiple tumor types.
Regorafenib (BAY 73-4506), a novel oral multikinase inhibitor, potently inhibits these endothelial cell kinases in biochemical and cellular kinase phosphorylation assays. Furthermore, regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-β, and fibroblast growth factor receptor 1) and the mutant oncogenic kinases c-KIT, RET, and B-RAF. The antiangiogenic effect of regorafenib was demonstrated in vivo by dynamic contrast-enhanced magnetic resonance imaging. Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts. In a daily (qd)×4 dosing study, the pharmacodynamic effects persisted for 48 hr after the last dosing and correlated with tumor growth inhibition (TGI). A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qd×5 dosing at 10 and 30 mg/kg. Regorafenib exhibited potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages observed in breast MDA-MB-231 and renal 786-O carcinoma models. Pharmacodynamic analyses of the breast model revealed strong reduction in staining of proliferation marker Ki-67 and phosphorylated extracellular regulated kinases 1/2. These data demonstrate that regorafenib is a well-tolerated, orally active multikinase inhibitor with a distinct target profile that may have therapeutic benefit in human malignancies
1. Chu E. An Update on the Current and Emerging Targeted Agents in Metastatic Colorectal Cancer. Clin Colorectal Cancer. 2011 Jul 11. [Epub ahead of print] PubMed PMID: 21752724.
2. Demetri GD. Differential properties of current tyrosine kinase inhibitors in gastrointestinal stromal tumors. Semin Oncol. 2011 Apr;38 Suppl 1:S10-9. Review. Erratum in: Semin Oncol. 2011 Jun;38(3):467. PubMed PMID: 21419931.
3. Wilhelm SM, Dumas J, Adnane L, Lynch M, Carter CA, Schütz G, Thierauch KH, Zopf D. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011 Jul 1;129(1):245-55. doi: 10.1002/ijc.25864. Epub 2011 Apr 22. PubMed PMID: 21170960.
To place an order online, simply browse to the product you are interested in and click on the 'Add to Cart' button. To complete this process, you will need to confirm the size and quantity of the products that you require.
To complete an order you will need to register using our simple online registration process. We do not share your contact details with any third parties.
When you are ready to check out simply enter your PO number to complete the ordering process. Please ensure that you send us a copy of your PO by fax or email afterwards. We will then liaise with you or your purchasing department to confirm the order.
Found your products but not ready to order?
Why not use our WishList feature to store lists of products? This convenient feature allows you to manage lists, append notes to products and share lists with co-workers or colleagues.
You can email or fax us your purchase order and we will place the order for you. You can also phone us to place the order. Our contact details are:
- Tel: 866-930-6790
- Fax: 323-606-8156
- Email: [email protected]
We require the following information to process your order:
- The catalog number for each product.
- Your email address or fax number.
- Your name and telephone number.
- Shipping address and billing address.
- Purchase order numbers.