| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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ASN007 (ASN-007) is a novel, potent, orally bioavailable and selective inhibitor of ERK1/2 with robust antitumor activity. It blocks ERK1/2 with an IC50 of 2 nM and the RAS/RAF/MEK/ERK (MAPK) signaling pathway. Regardless of the mutation's subtype, ASN007 exhibits strong preclinical activity in KRAS-driven models as well as BRAF mutant models, including melanoma resistant to RAF/MEK inhibitors.
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| ln Vitro |
In various cell lines, ERK-IN-3 prevents the phosphorylation of ERK1/2 substrates like RSK1, FRA1, and Elk1[1]. Single-digit nanomolar antiproliferative activity of ERK-IN-3 is specific for cancer cell lines that are MAPK pathway dependent[1].
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| ln Vivo |
At effective doses, ERK-IN-3 (daily p.o.) was well tolerated and inhibited tumor growth in several BRAF and KRAS mutant mouse xenograft models[1].
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| References | ||
| Additional Infomation |
ERK1/2 Inhibitor ERAS-007 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases 1 (ERK1) and 2 (ERK2), with potential antineoplastic activity. Upon oral administration, ERAS-007 specifically binds to and inhibits the serine/threonine-protein kinase activities of both ERK1 and ERK2, thereby preventing the phosphorylation of ERK1/2 substrates and the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent proliferation and survival of tumor cells. The MAPK/ERK pathway, also known as the RAS/RAF/MEK/ERK pathway, is hyperactivated in a variety of tumor cell types due to mutations in upstream targets. It plays a key role in the proliferation, differentiation and survival of tumor cells.
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| Molecular Formula |
C22H25CLFN7O2
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|---|---|
| Molecular Weight |
473.931006193161
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| Exact Mass |
473.17
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| Elemental Analysis |
C, 55.75; H, 5.32; Cl, 7.48; F, 4.01; N, 20.69; O, 6.75
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| CAS # |
2055597-12-9
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| Related CAS # |
ASN007 benzenesulfonate;2055597-39-0
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| PubChem CID |
124122366
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| Appearance |
White to light yellow solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
644
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CN=C(N=C1N2C=C(N=C2)C(=O)N[C@H](CN)C3=CC(=CC(=C3)Cl)F)NC4CCOCC4
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| InChi Key |
PWHIUQBBGPGFFV-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C22H25ClFN7O2/c1-13-10-26-22(28-17-2-4-33-5-3-17)30-20(13)31-11-19(27-12-31)21(32)29-18(9-25)14-6-15(23)8-16(24)7-14/h6-8,10-12,17-18H,2-5,9,25H2,1H3,(H,29,32)(H,26,28,30)/t18-/m1/s1
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| Chemical Name |
N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]imidazole-4-carboxamide;benzenesulfonic acid
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| Synonyms |
ASN007; ASN 007; ASN-007
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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) |
DMSO: 95 ~200 mg/mL (200.5~422 mM)
Ethanol: ~95 mg/mL (~200.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.39 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 20.8 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: ≥ 2.08 mg/mL (4.39 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 20.8 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: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 6.67 mg/mL (14.07 mM) in 0.5% MC 0.5% Tween-80 (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1100 mL | 10.5501 mL | 21.1002 mL | |
| 5 mM | 0.4220 mL | 2.1100 mL | 4.2200 mL | |
| 10 mM | 0.2110 mL | 1.0550 mL | 2.1100 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 |
| NCT03415126 | Completed | Drug: ASN007: ascending doses Drug: ASN007 RD |
Cancer Malignancy |
Asana BioSciences | January 19, 2018 | Phase 1 |
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