Gefitinib NEW
| Price | $36 | $1.2 |
| Package | 1kg | 1000kg |
| Min. Order: | 1kg |
| Supply Ability: | g-kg-tons, free sample is available |
| Update Time: | 2024-04-29 |
Product Details
| Product Name: Gefitinib | CAS No.: 184475-35-2 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: g-kg-tons, free sample is available | Release date: 2024/04/29 |
| Lead time: In stock, ready for shipment | Packaging: bag/bottle/drum/IBC |
| Delivery: By express, by air, by sea | Origin: Manufacturer, advantage product |
| COA, MSDS: Available, contact us for details | Name: Mia |
1. Materials information
| Name | gefitinib |
|---|---|
| Synonym | More Synonyms |
| Description | Gefitinib (ZD1839) is a EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells. |
|---|---|
| Related Catalog | Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR Research Areas >> Cancer |
| Target | EGFR |
| In Vitro | Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth[1]. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM[2]. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μM[3]. |
| In Vivo | Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts[3]. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation[4]. |
| Cell Assay | Cancer cells are seeded in 96-well plates and are treated with different doses of Gefitinib (0.01-20 μM), Metformin or both for 72 hours. Cell proliferation is measured with the MTT assay. The IC50 values are determined by interpolation from the dose-response curves. Results represent the median of 3 separate experiments each conducted in quadruplicate. The results of the combined treatment are analyzed according to the method of Chou and Talalay by using the CalcuSyn software program[3]. |
| Animal Admin | Mice[3] Four- to 6-week old female balb/c athymic (nu+/nu+) mice are acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that has been resuspended in 200 μL of Matrigel. When established tumors of approximately 75 mm3 in diameter are detected, mice are left untreated or treated with oral administrations of metformin (200 mg/mL metformin diluted in drinking water and present throughout the experiment), gefitinib (150 mg/kg daily orally by gavage), or both for the indicated time periods. Each treatment group consists of 10 mice. Tumor volume is measured using the formula π/6×larger diameter×(smaller diameter)2. Rats[4] The rats are randomly assigned to 1 of 4 experimental groups: 1) the unirradiated rats treated with oral administration of vehicle (0.1% Tween 80) once daily; 2) the unirradiated rats treated with oral administration of gefitinib (50 mg/kg/day) once daily; 3) the irradiated rats treated with oral administration of vehicle once daily; 4) the irradiated rats treated with oral administration of gefitinib once daily. Each experimental group comprised 5-6 rats and all treatments are delivered for 14 days. |
| References | [1]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23. [2]. Moasser MM, et al. The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8. [3]. Morgillo F, et al. Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19. [4]. Miyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85. [5]. Noh CK, et al. Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. J Sep Sci. 2017 Jul 27. [6]. Dhar D, et al. Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 586.8±50.0 °C at 760 mmHg |
| Melting Point | 119-1200C |
| Molecular Formula | C22H24ClFN4O3 |
| Molecular Weight | 446.902 |
| Flash Point | 308.7±30.1 °C |
| Exact Mass | 446.152100 |
| PSA | 68.74000 |
| LogP | 4.11 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.621 |
| Storage condition | Store at RT |
| Symbol |  GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302-H315-H319-H335 |
| Precautionary Statements | P301 + P312 + P330-P305 + P351 + P338 |
| Hazard Codes | Xi |
| Risk Phrases | R36/37/38:Irritating to eyes, respiratory system and skin . |
| Safety Phrases | S24/25 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
| RTECS | HP1149700 |
| HS Code | 29143900 |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
By Express
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
By Air
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
By Sea
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
4. Contact information
For more details, pls contact us freely.
Email address: mia@fdachem.com
Mob: 86 18336764634
WhatsApp/Skype/Wechat/LINE: 86 18336764634
Company Profile Introduction
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China
- Since: 2023-02-10
- Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro