MedKoo Cat#: 207046 | Name: ASN007 free base
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Description:

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

ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. with low single-digit nM IC50 values. ASN007 showed a slow dissociation rate (long target residence time) as compared to several other known ERK inhibitors. In mechanistic cell-based assays, ASN007 inhibited the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines. ASN007 showed single-digit nanomolar antiproliferative activity that was selective for MAPK-pathway dependent cancer cell lines.

Chemical Structure

ASN007 free base
ASN007 free base
CAS#2055597-12-9 (free base)

Theoretical Analysis

MedKoo Cat#: 207046

Name: ASN007 free base

CAS#: 2055597-12-9 (free base)

Chemical Formula: C22H25ClFN7O2

Exact Mass: 473.1742

Molecular Weight: 473.94

Elemental Analysis: C, 55.75; H, 5.32; Cl, 7.48; F, 4.01; N, 20.69; O, 6.75

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 1,950.00 Ready to ship
500mg USD 3,650.00 Ready to ship
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Related CAS #
2055596-76-2 (racemic) 2055597-12-9 (free base) 2055597-39-0 (besylate) 2055597-42-5 (HCl) 2055597-13-0 (R-isomer)
Synonym
ASN007; ASN-007; ASN 007;
IUPAC/Chemical Name
(S)-N-(2-amino-1-(3-chloro-5-fluorophenyl)ethyl)-1-(5-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1H-imidazole-4-carboxamide
InChi Key
PWHIUQBBGPGFFV-GOSISDBHSA-N
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
SMILES Code
CC1=CN=C(NC2CCOCC2)N=C1N3C=NC(C(N[C@H](CN)C4=CC(F)=CC(Cl)=C4)=O)=C3
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
Shelf Life
>3 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
Indeed, ASN007 showed much more potent activity against a broader panel of KRAS, NRAS, and HRAS mutant cell lines compared to other ERK1/2 inhibitors such as BVD-523 and GDC-0994. In a daily oral dosing regimen, ASN007 demonstrated strong inhibition of tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses. Of note, ASN007 also showed strong efficacy using various intermittent dosing regimens. ASN007 has a good pharmacokinetic profile in preclinical species and does not exhibit significant inhibition of CYP enzymes or hERG channel. IND-enabling studies are ongoing in preparation for a phase 1 clinical trial to evaluate oral ASN007 in patients with BRAF and K- , H- , and N-RAS mutant cancers
Biological target:
ERK-IN-3 is a potent inhibitor of ERK that inhibis ERK1/2 with low single-digit nM IC50 values.
In vitro activity:
In vivo activity:
Solvent mg/mL mM
Solubility
DMSO 200.0 421.99
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 473.94 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
1: Portelinha A, Thompson S, Smith RA, Da Silva Ferreira M, Asgari Z, Knezevic A, Seshan V, de Stanchina E, Gupta S, Denis L, Younes A, Reddy S. ASN007 is a selective ERK1/2 inhibitor with preferential activity against RAS-and RAF-mutant tumors. Cell Rep Med. 2021 Jul 21;2(7):100350. doi: 10.1016/j.xcrm.2021.100350. PMID: 34337566; PMCID: PMC8324497. 2: Ku BM, Heo JY, Kim J, Sun JM, Lee SH, Ahn JS, Park K, Ahn MJ. ERK inhibitor ASN007 effectively overcomes acquired resistance to EGFR inhibitor in non-small cell lung cancer. Invest New Drugs. 2022 Apr;40(2):265-273. doi: 10.1007/s10637-021-01121-6. Epub 2022 Jan 1. PMID: 34973117; PMCID: PMC8993753.