Sunitinib

Product name	Sunitinib
CAS	557795-19-4
Appearance	white powder
Assay	99%
Storage	Cool and Protect from light

Description:
Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. 

Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. 
 
Application:

Sunitinib malate, also called sunitinib, is a novel, oral, multi-targeted , small molecule oxindole tyrosine kinase inhibitor which inhibits multiple receptor tyrosine kinases including c-KIT, FLT3 kinase, colony-stimulating factor 1 receptor and RET kinase. The IC50 of sunitinib is approximately 10-20 ng/ml to NB cell lines, which is within the clinically relevant human trough serum concentration (50-100 ng/ml).
Receptor tyrosine kinases activated a number of different intracellular signaling pathways. 
In neuroblastoma (NB) cell lines, SKN-BE (2), NUB-7, SH-SY5Y and LAN-5, sunitinib significantly inhibited cell proliferation after a treatment for 48 hours, in a concentration-dependent manner. 

Treatment with 20, 30 or 40 mg/kg of sunitinib made NOD/SCID mice inoculated with xenograft tumor cells show significant reduction (P <0.05) in primary tumor growth (%T/C: 49% for SK-N-BE (2) and 55% for NB12 tumor, T/C: average treated tumor mass/average control tumor mass). Treatment with different doses of sunitinib (20, 30 or 40 mg/kg) for 14 days resulted in a dramatic decrease in the numbers and size of metastatic sites and a significant difference in liver weight in mice injected intravaneously with 106 SK-N-BE(2) cells for 7 days compared with the control group.

Packaging & Shipping

Company Information

   Hebei Lingding Biotechnology Co., Ltd. is a professional business company ,that include pharmaceutical raw materials, pharmaceutical intermediates,and other more than 1000 products of the enterprise,  The registered capital is 3 million yuan, it is a collection of scientific research, production and sales in one of the enterprises.

Since its establishment, the company has always adhered to the core concept of "focus on products, attentive service", adhere to the business purpose of "innovation, professional, win-win", to provide customers with a full range of meticulous and thoughtful services. We will adhere to the customer's serious and responsible attitude, comply with the standardized operation procedures, with efficient execution to complete customer needs.

The company's products are sold all over the world, mainly exported to the United States, Europe, Southeast Asia, Australia, the Middle East and South Africa and other countries.The company has a strong scientific research and technical team, can provide customers with high quality products and a full range of services. We will provide first-class products and better service to face the needs of customers, to meet the challenges of the market.  Welcome domestic and foreign customers to negotiate.
Our Services
 1.Any inquiry or message will be replied within 12 hours.
 2.Professional manufacturer. Welcome to visit our website.
 3.API, Intermediate are available, we can offer Custom Synthesis, and registration as well.
 4.Fast delivery.
 5.After-sale services
FAQ
 Q1. Are you a manufacturer?
Answer: Yes, we have our own factory.

Q2. Do you have GMP or DMF?
Answer: Yes, we have GMP certificate for some products, and we can provide DMF as well.

Q3. What information should I let you know if I want to get a quotation?
Answer: -Quality you require, eg. Assay, Purity, or single impurity
-Quantity you need
-Standard you want, such as USP, EP, JP etc.

Q4. How to make the payment?
Answer: T/T in advance are highly recommended. We can accept Western Union,
Money Gram and Paypal as well.

Q5. When will you deliver the goods?
Answer: For sample(less than 1kg), in about 3 working days after payment; for larger orders (more than 1kg), in about 7 working days after payment.

Q6. How will you deliver the goods?
Answer: We have strong cooperation with DHL, TNT, UPS, FEDEX, EMS, China Air Post. For container products, we can do sea shipping. You also can choose your own shipping forwarder.

Q7. When will we receive the goods?
Answer: For samples, we will send by TNT/DHL/FEDEX/UPS express, usually it takes about 3-5 to reach you; for larger orders, it will take about 7 -10days at most.

Q8. What if we find your products unsatisfied?
Answer: We will send you a COA (Certificate of Analysis) to you first for you to confirm the quality, but if you find our products not confirm with the COA after you receive it, please show us your test result, we will refund you once we confirm that.
 
Q9.Do you have stock?
Answer:As we know,most customers prefer stock,so we will try to keep stock for some products.