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MedKoo Cat#: 206463 | Name: Staurosporine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Staurosporine, also known as antibiotic AM-2282 or STS, is a potent, non-selective inhibitor of protein kinases, including protein kinase C with promising anti-cancer activity. Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. Staurosporine induces apoptosis in pancreatic carcinoma cells via the intrinsic signaling pathway. Staurosporine synergizes with the HER2 inhibitor lapatinib to restore sensitivity toward HER2 inhibition in a HER2 inhibitor resistant breast cancer model.

Chemical Structure

Staurosporine
CAS#62996-74-1

Theoretical Analysis

MedKoo Cat#: 206463

Name: Staurosporine

CAS#: 62996-74-1

Chemical Formula: C28H26N4O3

Exact Mass: 466.2005

Molecular Weight: 466.54

Elemental Analysis: C, 72.09; H, 5.62; N, 12.01; O, 10.29

Price and Availability

Size Price Availability Quantity
5mg USD 110.00 Ready to ship
10mg USD 180.00 Ready to Ship
25mg USD 350.00 Ready to ship
50mg USD 485.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to Ship
500mg USD 2,450.00 Ready to Ship
1g USD 3,850.00 Ready to Ship
2g USD 6,450.00 Ready to ship
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Related CAS #
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Synonym
AM-2282; AM2282; AM 2282; STS; Antibiotic 230; CGP 41251; CGP41251; CGP-41251; CGP-39360; CGP39360; CGP 39360; Staurosporine; Staurosporin.
IUPAC/Chemical Name
(5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14-one
InChi Key
HKSZLNNOFSGOKW-FYTWVXJKSA-N
InChi Code
InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
SMILES Code
CO[C@@H]1[C@@H](C[C@@H]2N3C4=C(N(C5=CC=CC=C56)[C@@]1(C)O2)C6=C7CNC(C7=C4C8=CC=CC=C83)=O)NC
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC50 of 3 μM.
In vitro activity:
The gene expression analysis through RT-qPCR (list of primers are provided in Table 1) shows that staurosporine treatment significantly induces the mRNA levels of ERN1, MOAP1, BAK1, Caspase-3, and Caspase 7 when compared to the untreated control group. These results suggest that staurosporine-mediated apoptosis in HEK293T cells largely depends upon ERN1, MOAP1, and BAK1, which may be the key initiator molecules for the apoptosis pathway in our model. Reference: PLoS One. 2022 Sep 26;17(9):e0275072. https://pubmed.ncbi.nlm.nih.gov/36156601/
In vivo activity:
PBS-injected non-ONI (optic nerve injury) control mouse retina had an average RGC cell number of 151.75 ± 12.01 in captured photos. In comparison with the control, this study found that by 30 days after the ONI, there was substantial reduction in the number of retinal ganglion cells. PBS-injected ONI retinas had an approximate 63.59% loss of RGC (remaining RGC 36.4 ± 9.55%; P<0.001). In contrast, STS (staurosporine) injection significantly promoted RGC survival by an approximate 25.54% compared with PBS injection (remaining RGC approximately 61.94 ± 6.91%; P<0.01). The above results prove that STS can act as a neuroprotectant for ganglion cells that would otherwise die from ONI-induced neurotoxicity. Reference: Int J Clin Exp Pathol. 2017 Jul 1;10(7):7920-7928. https://pubmed.ncbi.nlm.nih.gov/31966642/
Solvent mg/mL mM comments
Solubility
DMSO 43.9 94.19
Methanol 2.0 4.29
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 466.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Pandeya A, Khalko RK, Singh S, Kumar M, Gosipatala SB. Hcmv-miR-UL148D regulates the staurosporine-induced apoptosis by targeting the Endoplasmic Reticulum to Nucleus signaling 1(ERN1). PLoS One. 2022 Sep 26;17(9):e0275072. doi: 10.1371/journal.pone.0275072. PMID: 36156601; PMCID: PMC9512192. 2. Brunelli F, Torosantucci L, Gelmetti V, Franzone D, Grünewald A, Krüger R, Arena G, Valente EM. PINK1 Protects against Staurosporine-Induced Apoptosis by Interacting with Beclin1 and Impairing Its Pro-Apoptotic Cleavage. Cells. 2022 Feb 15;11(4):678. doi: 10.3390/cells11040678. PMID: 35203326; PMCID: PMC8870463. 3. Kim YH, Gum SI, Lee TY, Shin JY, Ma JY, Kim I, Park YJ, Jung JC. The neuroprotective effect of staurosporine on mouse retinal ganglion cells after optic nerve injury. Int J Clin Exp Pathol. 2017 Jul 1;10(7):7920-7928. PMID: 31966642; PMCID: PMC6965234. 4. Tagliati F, Gagliano T, Gentilin E, Minoia M, Molè D, Delgi Uberti EC, Zatelli MC. Magmas overexpression inhibits staurosporine induced apoptosis in rat pituitary adenoma cell lines. PLoS One. 2013 Sep 17;8(9):e75194. doi: 10.1371/journal.pone.0075194. Erratum in: PLoS One. 2013 Sep 27;8(9):null. PMID: 24069394; PMCID: PMC3775776.
In vitro protocol:
1. Pandeya A, Khalko RK, Singh S, Kumar M, Gosipatala SB. Hcmv-miR-UL148D regulates the staurosporine-induced apoptosis by targeting the Endoplasmic Reticulum to Nucleus signaling 1(ERN1). PLoS One. 2022 Sep 26;17(9):e0275072. doi: 10.1371/journal.pone.0275072. PMID: 36156601; PMCID: PMC9512192. 2. Brunelli F, Torosantucci L, Gelmetti V, Franzone D, Grünewald A, Krüger R, Arena G, Valente EM. PINK1 Protects against Staurosporine-Induced Apoptosis by Interacting with Beclin1 and Impairing Its Pro-Apoptotic Cleavage. Cells. 2022 Feb 15;11(4):678. doi: 10.3390/cells11040678. PMID: 35203326; PMCID: PMC8870463.
In vivo protocol:
1. Kim YH, Gum SI, Lee TY, Shin JY, Ma JY, Kim I, Park YJ, Jung JC. The neuroprotective effect of staurosporine on mouse retinal ganglion cells after optic nerve injury. Int J Clin Exp Pathol. 2017 Jul 1;10(7):7920-7928. PMID: 31966642; PMCID: PMC6965234. 2. Tagliati F, Gagliano T, Gentilin E, Minoia M, Molè D, Delgi Uberti EC, Zatelli MC. Magmas overexpression inhibits staurosporine induced apoptosis in rat pituitary adenoma cell lines. PLoS One. 2013 Sep 17;8(9):e75194. doi: 10.1371/journal.pone.0075194. Erratum in: PLoS One. 2013 Sep 27;8(9):null. PMID: 24069394; PMCID: PMC3775776.
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PMID: 39477806. 4: Binjubair FA, Almansour BS, Ziedan NI, Abdel-Aziz AA, Al-Rashood ST, Elgohary MK, Elkotamy MS, Abdel-Aziz HA. Molecular docking, DFT and antiproliferative properties of 4-(3,4-dimethoxyphenyl)-3-(4-methoxyphenyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridine as potent anticancer agent with CDK2 and PIM1 inhibition potency. Drug Dev Res. 2024 Nov;85(7):e70009. doi: 10.1002/ddr.70009. PMID: 39467111. 5: Arito M, Tsutiya A, Sato M, Omoteyama K, Sato T, Motonaga Y, Suematsu N, Kurokawa MS, Kato T. Role of layilin in regulating mitochondria-mediated apoptosis: a study on B cell lymphoma (BCL)-2 family proteins. BMC Mol Cell Biol. 2024 Oct 25;25(1):24. doi: 10.1186/s12860-024-00521-9. PMID: 39455917; PMCID: PMC11515419. 6: Chen RY, Ding LJ, Liu YJ, Shi JJ, Yu J, Li CY, Lu JF, Yang GJ, Chen J. Marine Staurosporine Analogues: Activity and Target Identification in Triple-Negative Breast Cancer. Mar Drugs. 2024 Oct 5;22(10):459. doi: 10.3390/md22100459. PMID: 39452867; PMCID: PMC11509616. 7: Popović L, Brankatschk B, Palladino G, Rossner MJ, Wehr MC. Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. Biomed Pharmacother. 2024 Nov;180:117523. doi: 10.1016/j.biopha.2024.117523. Epub 2024 Oct 14. PMID: 39405910. 8: Yang R, Lai C, Huang L, Li F, Peng W, Wu M, Xin J, Lu Y, Ouyang M, Bai Y, Lei H, He S, Lin Y. Role of disulfidptosis in colorectal adenocarcinoma: implications for prognosis and immunity. Front Immunol. 2024 Sep 27;15:1409149. doi: 10.3389/fimmu.2024.1409149. PMID: 39399504; PMCID: PMC11466812. 9: Carranza-Aranda AS, Jave-Suárez LF, Flores-Hernández FY, Huizar-López MDR, Herrera-Rodríguez SE, Santerre A. In silico and in vitro study of FLT3 inhibitors and their application in acute myeloid leukemia. Mol Med Rep. 2024 Dec;30(6):229. doi: 10.3892/mmr.2024.13353. Epub 2024 Oct 11. 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RSC Adv. 2024 Sep 24;14(41):30346-30363. doi: 10.1039/d4ra04036h. PMID: 39318461; PMCID: PMC11420776. 15: Li H, Hu W, Wu Z, Tian B, Ren Y, Zou X. Esketamine improves cognitive function in sepsis-associated encephalopathy by inhibiting microglia-mediated neuroinflammation. Eur J Pharmacol. 2024 Nov 15;983:177014. doi: 10.1016/j.ejphar.2024.177014. Epub 2024 Sep 21. PMID: 39312992. 16: Borek WE, Nobre L, Pedicona SF, Campbell AE, Christopher JA, Nawaz N, Perkins DN, Moreno-Cardoso P, Kelsall J, Ferguson HR, Patel B, Gallipoli P, Arruda A, Ambinder AJ, Thompson A, Williamson A, Ghiaur G, Minden MD, Gribben JG, Britton DJ, Cutillas PR, Dokal AD. Phosphoproteomics predict response to midostaurin plus chemotherapy in independent cohorts of FLT3-mutated acute myeloid leukaemia. EBioMedicine. 2024 Oct;108:105316. doi: 10.1016/j.ebiom.2024.105316. Epub 2024 Sep 17. 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