Saracatinib (AZD0530) | CAS:379231-04-6

Saracatinib (AZD0530)

ChemFaces products have been cited in many studies from excellent and top scientific journals

Order & Inquiry & Tech Support

Tel: (0086)-27-84237683
Tech: service@chemfaces.com
Order: manager@chemfaces.com
Address: 176, CheCheng Eest Rd., WETDZ, Wuhan, Hubei 430056, PRC

How to Order

Orders via your E-mail:

1. Product number / Name / CAS No.
2. Delivery address
3. Ordering/billing address
4. Contact information
Order: manager@chemfaces.com

Delivery time

Delivery & Payment method

1. Usually delivery time: Next day delivery by 9:00 a.m. Order now

2. We accept: Wire transfer & Credit card & Paypal

Citing Use of our Products

More Impact Factor than five Cite...

* Packaging according to customer requirements(5mg, 10mg, 20mg and more). We shipped via FedEx, DHL, UPS, EMS and others courier.

According to end customer requirements, ChemFaces provide solvent format. This solvent format of product intended use: Signaling Inhibitors, Biological activities or Pharmacological activities.

Size /Price /Stock	10 mM * 1 mL in DMSO / Inquiry
Other Packaging	*Packaging according to customer requirements(100uL/well, 200uL/well and more), and Container use Storage Tube With Screw Cap

Featured Products

More...

Oxoglaucine

Catalog No: CFN90508
CAS No: 5574-24-3
Price: $318/5mg

Ginsenoside Rk1

Catalog No: CFN92644
CAS No: 494753-69-4
Price: $188/20mg

Hydroxysafflor yellow A

Catalog No: CFN99950
CAS No: 78281-02-4
Price: $60/20mg

Rutaecarpine

Catalog No: CFN97337
CAS No: 84-26-4
Price: $40/20mg

Isocorynoxeine

Catalog No: CFN98155
CAS No: 51014-29-0
Price: $128/20mg

Punicalagin

Catalog No: CFN99938
CAS No: 65995-63-3
Price: $108/20mg

Parishin E

Catalog No: CFN93115
CAS No: 952068-57-4
Price: $298/20mg

Cantharidin

Catalog No: CFN99790
CAS No: 56-25-7
Price: $40/20mg

epsilon-Viniferin

Catalog No: CFN97067
CAS No: 62218-08-0
Price: $338/10mg

Phytic acid

Catalog No: CFN99792
CAS No: 83-86-3
Price: $40/20mg

Description:

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy.

Targets:

Src | Autophagy

In vitro:

Mol Cancer Res,2009 Apr;7(4):476-88.

The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts.[Pubmed: 19372577]

Tumor cells in the bone microenvironment are able to initiate a vicious cycle of bone degradation by mobilizing osteoclasts, multinucleated cells specialized in bone degradation. c-Src is highly expressed both in tumors and in osteoclasts. Therefore, drugs like AZD0530, designed to inhibit Src activity, could selectively interfere with both tumor and osteoclast activity.
METHODS AND RESULTS:
Here we explored the effects of AZD0530 on human osteoclast differentiation and activity. The effect on osteoclasts formed in vivo was assessed in mouse fetal calvarial explants and in isolated rabbit osteoclasts, where it dose-dependently inhibited osteoclast activity. Its effect on formation and activity of human osteoclasts in vitro was determined in cocultures of human osteoblasts and peripheral blood mononuclear cells. AZD0530 was most effective in inhibiting osteoclast-like cell formation when present at the onset of osteoclastogenesis, suggesting that Src activity is important during the initial phase of osteoclast formation. Formation of active phosphorylated c-Src, which was highly present in osteoclast-like cells in cocultures and in peripheral blood mononuclear cell monocultures, was significantly reduced by AZD0530. Furthermore, it reversibly prevented osteoclast precursor migration from the osteoblast layer to the bone surface and subsequent formation of actin rings and resorption pits.
CONCLUSIONS:
These data suggest that Src is pivotal for the formation and activity of human osteoclasts, probably through its effect on the distribution of the actin microfilament system. The reversible effect of AZD0530 on osteoclast formation and activity makes it a promising candidate to temper osteoclastic bone degradation in bone diseases with enhanced osteoclast activity such as osteolytic metastatic bone disease.

In vivo:

Mol Oncol,2009 Jun;3(3):248-61.

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.[Pubmed: 19393585]

METHODS AND RESULTS:
AZD0530, an orally available Src inhibitor, demonstrated potent antimigratory and anti-invasive effects in vitro, and inhibited metastasis in a murine model of bladder cancer. Antiproliferative activity of AZD0530 in vitro varied between cell lines (IC(50) 0.2 ->10μM). AZD0530 inhibited tumor growth in 4/10 xenograft models tested and dynamically inhibited in vivo phosphorylation of Src substrates paxillin and FAK in both growth-inhibition-resistant and -sensitive xenografts. The activity of AZD0530 in NBT-II bladder cancer cells in vitro was consistent with inhibition of cell migration and stabilization of cell-cell adhesion.
CONCLUSIONS:
These data suggest a dominant anti-invasive pharmacology for AZD0530 that may limit tumor progression in a range of cancers. AZD0530 is currently in Phase II clinical trials.

Saracatinib (AZD0530) Description

Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Cell Research:

Oncogene,2008 Oct 23;27(49):6365-75.

Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530.[Pubmed: 18679417]

Cell lines:PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 and RWPE-1 cells
Concentrations: 62.5 nM - 16 mM
Incubation Time: 1, 3 and 5 days
Method:
Cells are seeded at a density of 2× 103 in 96-well plates and incubated overnight. Then Saracatinib (62.5 nM-16 mM) is added to the cells. After 1, 3 and 5 days, culture medium is removed followed by addition of 0.2 mL DMSO per well and continuous shaking of plates at 200 rotations per minute for 15min. Then IC50 is measured by MTT metho.

Animal Research:

Oncogene,2008 Oct 23;27(49):6365-75.

Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530.[Pubmed: 18679417]

Animal Models: CB17 mice are implanted with DU145 cells.
Dosages:25 mg/kg
Administration: Orally administered daily

Product Name	Saracatinib (AZD0530)
Price:
CAS No.:	379231-04-6
Catalog No.:	CFN60031
Molecular Formula:	C₂₇H₃₂ClN₅O₅
Molecular Weight:	542.03 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS
Similar structural:	Comparison
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library Src Inhibitor Library Autophagy Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	1.8449 mL	9.2246 mL	18.4492 mL	36.8983 mL	46.1229 mL
5 mM	0.369 mL	1.8449 mL	3.6898 mL	7.3797 mL	9.2246 mL
10 mM	0.1845 mL	0.9225 mL	1.8449 mL	3.6898 mL	4.6123 mL
50 mM	0.0369 mL	0.1845 mL	0.369 mL	0.738 mL	0.9225 mL
100 mM	0.0184 mL	0.0922 mL	0.1845 mL	0.369 mL	0.4612 mL

CFN80292	d-chiro-Inositol	643-12-9	180.2	C₆H₁₂O₆
CFN95186	Bergaptol-beta-glucopyranoside	131623-13-7	364.3	C₁₇H₁₆O₉
CFN70268	(1R)-Chrysanthemolactone	14087-70-8	168.2	C₁₀H₁₆O₂
CFN92795	Yukovanol	76265-12-8	354.5	C₂₀H₁₈O₆