Staurosporine
DataSheet
Cat.No.£º
IC-012066
Product Information
Biological Activity
Staurosporine (antibiotic AM-2282 or STS) is a therapeutic agent that inhibits tumor cell growth by inducing cell death via intrinsic apoptotic pathways. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, though with little selectivity. Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, MLCK, CAM PKII, cdc2, v-Src, Lyn, c-Fgr and Syk with IC50 values of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM and 16 nM respectively. Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. Moreover, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species
Mouse
Rat
Rabbit
Guinea pig
Hamster
Dog
Weight (kg)
0.02
0.15
1.8
0.4
0.08
10
Body Surface Area (m2)
0.007
0.025
0.15
0.05
0.02
0.5
Km factor
3
6
12
8
5
20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Chemical Information
Molecular Weight
466.53
Formula
C28H26N4O3
CAS Number
62996-74-1
Purity
>98%
Solubility
>DMSO 10mg/mL
Storage
at -20¡ãC
Cell lines
A31 cell lines, CHO-KDR cell lines, Mo-7e cell lines and A431 cell lines.
Preparation method
The solubility of this compound in DMSO is <10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ¡ãC for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20¡ãC for several months.
Reaction Conditions
24 h; IC50=0.08 mM (A31 cell lines), IC50=0.30 mM (Mo-7e cell lines), IC50=1.0 mM (CHO-KDR cell lines).
Applications
Staurosporine inhibited the ligand-induced autophosphorylation of the receptors for platelet-derived growth factor (PDGF) (IC50=0.08 mM) in A31 cell lines, stem cell factor (c-Kit, IC50=0.30 mM) in Mo-7e cell lines, and for VEGF (KDR, IC50=1.0 mM) in CHO-KDR cell lines, but did not affect the ligand-induced autophosphorylation of the receptors for insulin, IGF-I, or epidermal growth factor (EGF) in A431 cell lines.
Animal models
Athymic nude mice
Dosage form
75 mg/kg/day; oral taken.
Applications
The treatment with Staurosporine (75 mg/kg/day p.o.) completely inhibits the angiogenic response to VEGF, but not to bFGF. Thus, Staurosporine may suppress tumor growth by inhibiting tumor angiogenesis (via its effects on the VEGF-R tyrosine kinases) in addition to directly inhibiting tumor cell proliferation (via its effects on PKCs). This anti-angiogenic action may contribute to the antimetastatic and broad antitumor activity displayed by Staurosporine, as well as the synergy with cytotoxic agents.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References
[1] Andrejauskas-Buchdunger E, Regenass U. Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251[J]. Cancer research, 1992, 52(19): 5353-5358.
[2] Fabbro D, Buchdunger E, Wood J, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent[J]. Pharmacology & therapeutics, 1999, 82(2): 293-301.
Order Information
Cell experiment:
Animal experiment:
|
Product Name |
Cat.No. |
Quantity |
Price($) |
Price($) |
Availability |
|
Staurosporine |
IC-012066 |
1mg |
$112.00 |
€93.33 |
In stock |
|
Staurosporine |
IC-012066 |
2mg |
$162.00 |
€135.00 |
In stock |
|
Staurosporine |
IC-012066 |
5mg |
$420.00 |
€350.00 |
In stock |
