| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
PKA[1]
PKA (cAMP-dependent protein kinase). |
|---|---|
| ln Vitro |
8-Bromo-cAMP (0.1/0.5 mM) can enhance the reprogramming efficiency of human neonatal foreskin fibroblasts (HFF1) cells, and 0.1 mM 8-Bromo-cAMP has a synergistic effect with valproic acid (0.5 mM) [1]. 8-Bromo-cAMP (20 μM, 24 and 48 hours) induces apoptosis of esophageal cancer cell line (Eca-109) [2]. 8-Bromo-cAMP (0.5 mM, 2 days) induces decidualization of human endometrial stromal cells [3].
In vitro, 8-Bromo-cAMP (0.1-0.5 mM) enhances the reprogramming efficiency of human neonatal foreskin fibroblast (HFF1) cells, showing synergy with valproic acid (0.5 mM). At 20 uM for 24-48 hours, it induces apoptosis in the esophageal cancer cell line Eca-109. At 0.5 mM for 2 days, it induces decidualization of human endometrial stromal cells. It inhibits growth, decreases proliferation, increases differentiation, and induces apoptosis of cancer cells via activation of the cAMP/PKA pathway. |
| ln Vivo |
8-Bromo-cAMP (60 mg/kg/day, intraperitoneal injection, 7 days) can reduce tumor growth in mice bearing CT26 tumors[4].
8-Bromo-cAMP (60 mg/kg/day, i.p., 7 days) reduces primary CRC tumor nodules and liver metastases in CT26 tumor-bearing mice. It inhibits vasculogenic mimicry (PAS-CD31 staining of colorectal and intestinal tumors) and angiogenesis. The compound inhibits cAMP and VEGF expression while increasing PKA expression in tumor tissues. It activates Erk1/2 via a Shc-independent pathway in certain cell types. |
| Enzyme Assay |
The binding affinity and selectivity of 8-Bromo-cAMP were assessed using competitive binding assays against native cAMP for PKA regulatory subunits. Radio-labeled cAMP displacement assays were performed using purified PKA holoenzyme or RI/RII regulatory subunits to determine binding affinity. Phosphodiesterase (PDE) resistance assays were conducted by incubating 8-Bromo-cAMP with recombinant PDE isoforms, followed by HPLC or LC-MS quantification to confirm its stability against enzymatic hydrolysis compared to native cAMP.
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| Cell Assay |
For apoptosis studies, Eca-109 esophageal cancer cells were treated with 8-Bromo-cAMP (20 uM) for 24 and 48 hours, then apoptotic markers were evaluated via Annexin V/PI double staining flow cytometry. Human neonatal foreskin fibroblast (HFF1) cells were treated with 0.1-0.5 mM 8-Bromo-cAMP for reprogramming efficiency assessment. Human endometrial stromal cells (HESCs) were exposed to 8-Bromo-cAMP (0.5 mM) for 2 days to induce decidualization, confirmed by morphology changes and prolactin secretion assays.
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| Animal Protocol |
Animal/Disease Models: CT26 tumor mice[4]
Doses: 60 mg/kg/day Route of Administration: i.p., 7 days Experimental Results: Decreases amounts of primary CRC tumor nodules and liver metastases. Reduces vasculogenic mimicry (PAS–CD31 staining of colorectal and intestinal tumors). Inhibits cAMP and VEGF expression, increases expression of PKA in tumor tissues. CT26 tumor-bearing mice were administered 8-Bromo-cAMP at 60 mg/kg/day via intraperitoneal (i.p.) injection for 7 consecutive days. Following treatment, primary CRC tumor nodules and liver metastases were counted and weighed. Vasculogenic mimicry was evaluated by PAS-CD31 double staining of colorectal and intestinal tumor sections. Tumor tissue lysates were analyzed for cAMP, VEGF, and PKA expression levels by ELISA or Western blotting. |
| ADME/Pharmacokinetics |
PK parameters of 8-Bromo-cAMP have not been extensively reported in independent standard databases. As a membrane-permeable and PDE-resistant cAMP analog, it exhibits significantly prolonged intracellular half-life compared to native cAMP. Solubility data shows it is soluble in H2O (4.11 mg/mL, ~10.07 mM) with adjustment to pH 7 with 1 M NaOH and heating to 60degC. Powder form should be stored at -20degC for up to 3 years, and in-solvent solutions at -80degC for 6 months.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data is available for this research compound. Standard laboratory safety precautions should be followed when handling. The compound is classified as for research use only and not for human or veterinary use. Animal studies using doses of 60 mg/kg/day for 7 days did not report any overt toxicity or treatment-related mortality in mice, but long-term toxicity assessments have not been conducted.
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| References |
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| Additional Infomation |
8-bromo-cAMP is a 3',5'-cyclic purine nucleotide, a compound of 3',5'-cyclic AMP with a bromine substituent at the 8-position of the adenine ring. It is an activator of cyclic AMP-dependent protein kinases but is not readily degraded by cyclic AMP phosphodiesterases. It has antidepressant and protein kinase agonist effects. It is a 3',5'-cyclic purine nucleotide, an organic bromine compound, and an adenylate ribonucleotide. Functionally related to 3',5'-cyclic AMP, it is a long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinases but is not readily degraded by cyclic AMP phosphodiesterases.
8-Bromo-cAMP is a widely used PKA activator with critical roles in studying cAMP signaling pathways. It has anti-proliferative and apoptotic effects against cancer cells. The compound activates Erk1/2 via a Shc-independent pathway and protects neutrophils against TNF-alpha-induced apoptosis. It is used in stem cell research to enhance the induction of pluripotency in human fibroblast cells. This compound is strictly for laboratory research use, has not entered clinical trials for therapeutic applications, and is not approved by any regulatory agency as a human drug. |
| Molecular Formula |
C10H11BRN5O6P
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|---|---|
| Molecular Weight |
408.1
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| Exact Mass |
406.963
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| CAS # |
23583-48-4
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| PubChem CID |
32014
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| Appearance |
Solid powder ; Off-white to light yellow
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| Density |
2.8 g/cm3
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| Boiling Point |
741.9ºC at 760 mmHg
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| Melting Point |
254ºC (dec.)(lit.)
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| Flash Point |
402.5ºC
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| Vapour Pressure |
4.12E-23mmHg at 25°C
|
| Index of Refraction |
2.037
|
| LogP |
0.526
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
532
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1[C@@H]2[C@H]([C@H]([C@@H](O2)N3C4=NC=NC(=C4N=C3Br)N)O)OP(=O)(O1)O
|
| InChi Key |
DVKQVRZMKBDMDH-UUOKFMHZSA-N
|
| InChi Code |
InChI=1S/C10H11BrN5O6P/c11-10-15-4-7(12)13-2-14-8(4)16(10)9-5(17)6-3(21-9)1-20-23(18,19)22-6/h2-3,5-6,9,17H,1H2,(H,18,19)(H2,12,13,14)/t3-,5-,6-,9-/m1/s1
|
| Chemical Name |
(4aR,6R,7R,7aS)-6-(6-amino-8-bromopurin-9-yl)-2-hydroxy-2-oxo-4a,6,7,7a-tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinin-7-ol
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| Synonyms |
8-Br-Camp
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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 |
| 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) |
H2O : ~5.74 mg/mL (~14.07 mM; ultrasonic and warming and adjust pH to 9 with 1 M NaOH and heat to 60°C)
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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 | 2.4504 mL | 12.2519 mL | 24.5038 mL | |
| 5 mM | 0.4901 mL | 2.4504 mL | 4.9008 mL | |
| 10 mM | 0.2450 mL | 1.2252 mL | 2.4504 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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