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Purity: ≥98%
BI-847325 (BI847325) is a novel, potent, orally bioavailable, and selective dual inhibitor of MEK (mitogen-activated protein kinase kinase) and Aurora kinase with potential antitumor activity. It inhibits Aurora B, human Aurora A, Aurora C, MEK1 and MEK2 with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM, respectively. BI 847325 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.
| ln Vitro |
BI 847325 prevents X from acting. It also inhibits human AK-A and AK-C, with IC50 values of 25 and 15 nM, respectively. laevis AK-B. Additionally, human MEK1 and MEK2 are inhibited by BI 847325, with IC50 values of 25 and 4 nM, respectively. BI 847325 LCK, MAP3K8, FGFR1, AMPK, CAMK1D, and TBK1 at 1000 nM; only LCK (5 nM) and MAP3K8 (93 nM) had IC50 values less than 100 nM. A375 and Calu-6 cell lines are inhibited by BI 847325, with GI50 values of 7.5 nM and 60 nM, respectively[1].
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| ln Vivo |
Oral administration of BI 847325 at a dose of 10 mg/kg per day proved effective in BRAF and KRAS mutant xenograft tumor models. When given once a week at a dose of 70 mg/kg, BI 847325 suppresses AK and MEK in cancers with KRAS mutations [1].
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| References |
[1]. Sini P, et al. Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases. Mol Cancer Ther. 2016 Oct;15(10):2388-2398
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| Molecular Formula |
C29H28N4O2
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| Molecular Weight |
464.56
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| CAS # |
1207293-36-4
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| SMILES |
O([H])C1=C(/C(/C2C([H])=C([H])C([H])=C([H])C=2[H])=N/C2C([H])=C([H])C(=C([H])C=2[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])C2C([H])=C([H])C(C#CC(N([H])C([H])([H])C([H])([H])[H])=O)=C([H])C=2N1[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2-hydroxyethyl cellulose, polysorbate 80 with pH adjusted to 2.8 with 1 M HCl:30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1526 mL | 10.7629 mL | 21.5257 mL | |
| 5 mM | 0.4305 mL | 2.1526 mL | 4.3051 mL | |
| 10 mM | 0.2153 mL | 1.0763 mL | 2.1526 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01324830 | Completed Has Results | Drug: day 1 to day 5 Drug: day 1 to day 14 |
Neoplasms | Boehringer Ingelheim | April 15, 2011 | Phase 1 |
The dual MEK and Aurora kinase inhibitor BI-847325 blocks the growth and survival of BRAF-mutant melanoma cell lines through induction of apoptosis.Mol Cancer Ther.2015 Jun;14(6):1354-64. |
BI-847325 induces apoptosis altering the expression of pro and anti-apoptotic proteins.Mol Cancer Ther.2015 Jun;14(6):1354-64. |
Decreased expression of Mcl-1 is required for BI-847325-mediated apoptosis.Mol Cancer Ther.2015 Jun;14(6):1354-64. |
BI-847325-mediated apoptosis is induced following downregulation of Mcl-1.Mol Cancer Ther.2015 Jun;14(6):1354-64. |
BI-847325 leads to decreased MEK expression inBRAF-mutant naïve and vemurafenib-resistant cells.Mol Cancer Ther.2015 Jun;14(6):1354-64. |
BI-847325 inhibits growth ofBRAF-mutant melanoma xenografts.Mol Cancer Ther.2015 Jun;14(6):1354-64. |
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