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| Targets |
Stauprimide is a small molecule that primes embryonic stem cells (ESCs) for differentiation. Its molecular target is NME2, a c-Myc-activating transcription factor. Stauprimide binds to NME2 and inhibits its nuclear translocation, thereby downregulating c-Myc expression. c-Myc is an oncogene that plays a key role in tumorigenesis and stem cell pluripotency. By inhibiting NME2 and c-Myc, Stauprimide promotes ESC differentiation and has potential anticancer applications. It is a selective inhibitor of protein kinase C.
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| ln Vitro |
Staupride (10 μM; 6 hours) decreases MYC levels by 15% to over 90% and inhibits MYC transcription in the majority of cell lines, with an EC50 range from 30 nM to 8 μM [1]. Staupride (2–8 μM; 24-72 hours) inhibits MYC, which stops cell growth in vitro; in RXF 393 cells, its IC50 is 780 nM [1]. Staupride (5 μM; 3 hours) decreases NME2 nuclear translocation, which prevents MYC transcription [1]. In several cell lines, staupride (4–10 μM; 6 hours) exhibits variable EC50s and diverse degrees of maximum MYC mRNA downregulation [1].
In vitro, Stauprimide dramatically primes embryonic stem cells for differentiation. It increases the efficiency of directed differentiation of mouse and human ESCs in vitro. The compound interacts with NME2 and inhibits its nuclear translocation, leading to downregulation of c-Myc transcription. Its in vitro activity is characterized by potent induction of ESC differentiation. Stauprimide is used as a research tool to study stem cell biology and differentiation. It also exhibits potential anticancer activity. |
| ln Vivo |
Oral staupride (50 mg/kg; once daily; days 30, 55) inhibits MYC transcription in RXF 393 tumors, decreases MYC protein levels in mice receiving RXF 393 or CAKI-1 cell xenografts, and stops tumor growth [1].
In vivo studies of Stauprimide are limited, but the compound has potential applications in regenerative medicine and cancer research. As an inducer of ESC differentiation, it may be used to generate differentiated cell types for transplantation or disease modeling. Its ability to downregulate c-Myc, an oncogene, suggests potential anticancer applications. However, detailed in vivo efficacy data for specific disease models are not widely available. Stauprimide is primarily used as a research tool. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Stauprimide typically involve measuring its binding to NME2, its molecular target. Surface plasmon resonance (SPR) or other binding assays can be used to determine the binding affinity. Stauprimide interacts with NME2 and inhibits its nuclear localization. These assays confirm the compound's mechanism of action as an NME2 inhibitor. The compound's selectivity for NME2 over other targets can also be assessed.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: Renal cancer cell line RXF 393 Cell Tested Concentrations: 2 μM, 4 μM, 8 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: 2-8 μM concentration inhibited cell proliferation. Western Blot Analysis[1] Cell Types: Renal cancer cell line RXF 393 cells and CAKI-1 cells Tested Concentrations: 5 μM Incubation Duration: 3 hrs (hours) Experimental Results: diminished nuclear localization of NME2. RT-PCR[1] Cell Types: CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells Tested Concentrations: 4μM, 6μM, 8μM, 10μM Incubation Duration: 6 hrs (hours) Experimental Results: Inhibition of KG1A cells MYC transcription, EC50 is 400±50 nM, inhibition rate is 90%; CA46 cells are resistant to stauprimide. In vitro cellular assays for Stauprimide typically involve treating embryonic stem cells (ESCs) with the compound and measuring differentiation markers. The compound dramatically primes ESCs for differentiation and increases the efficiency of directed differentiation. Its effects on NME2 localization and c-Myc expression can be assessed using immunofluorescence and Western blotting. These cell-based studies demonstrate the compound's ability to promote ESC differentiation and downregulate c-Myc. |
| Animal Protocol |
Animal/Disease Models: Xenograft tumor model of RXF 393 and CAKI-1 cells in NOD/SCID (severe combined immunodeficient) mouse [1]
Doses: 50 mg/kg Route of Administration: Oral; Route of Administration: Oral. 50 mg/kg; one time/day; days 30, 55 Experimental Results: Tumor growth was blocked in mice injected with RXF 393 or CAKI-1 cells during the dosing period. In vivo animal models for Stauprimide may include models of cancer where c-Myc is overexpressed, or models of regenerative medicine where stem cell differentiation is desired. The compound is administered by appropriate routes, and its effects on tumor growth or tissue regeneration are measured. However, detailed animal protocol information for Stauprimide is limited in the available literature. The compound is primarily used as a research tool for studying stem cell biology and c-Myc regulation. |
| ADME/Pharmacokinetics |
Stauprimide is a staurosporine analog with a molecular formula of C35H28N4O5 and a molecular weight of 584.62 g/mol. It is a semi-synthetic analogue of the staurosporine family of indolocarbazoles. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in both in vitro and in vivo studies. Stauprimide's solubility and formulation for administration should be optimized based on specific experimental requirements.
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| Toxicity/Toxicokinetics |
Stauprimide is a staurosporine analog that promotes embryonic stem cell differentiation. As with any compound that modulates cell differentiation and gene expression, potential toxicity may include effects on normal cellular function and development. The compound's safety profile should be evaluated in preclinical toxicology studies. Stauprimide is for research use only and is not approved for human therapeutic use. It represents a valuable tool compound for studying stem cell biology and c-Myc regulation.
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| References | |
| Additional Infomation |
Stauprimide (CAS# 154589-96-5) is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. It binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, leading to the downregulation of MYC transcription. Stauprimide is a non-broad spectrum inhibitor that interacts with NME2 (PUF) transcription factor to down-regulate c-Myc expression. It increases the efficiency of directed differentiation of mouse and human ESCs in vitro. The compound is for research use only and is not approved for human therapeutic use.
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| Molecular Formula |
C35H28N4O5
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| Molecular Weight |
584.63
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| Exact Mass |
584.205
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| CAS # |
154589-96-5
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| PubChem CID |
46245328
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
145°C
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| Index of Refraction |
1.783
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| LogP |
6.13
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
44
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| Complexity |
1220
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)C(=O)NC6=O)N(C)C(=O)C9=CC=CC=C9)OC
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| InChi Key |
MQCCJEYZKWZQHU-MPRCCEKMSA-N
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| InChi Code |
InChI=1S/C35H28N4O5/c1-35-31(43-3)23(37(2)34(42)18-11-5-4-6-12-18)17-24(44-35)38-21-15-9-7-13-19(21)25-27-28(33(41)36-32(27)40)26-20-14-8-10-16-22(20)39(35)30(26)29(25)38/h4-16,23-24,31H,17H2,1-3H3,(H,36,40,41)/t23-,24-,31-,35+/m1/s1
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| Chemical Name |
N-[(2S,3R,4R,6R)-3-methoxy-2-methyl-16,18-dioxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide
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| Synonyms |
N-Benzoyl-7-oxostaurosporine; Stauprimide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7105 mL | 8.5524 mL | 17.1048 mL | |
| 5 mM | 0.3421 mL | 1.7105 mL | 3.4210 mL | |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7105 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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