Eras-4001 |
Catalog No.GC79244
One-Click Copy Product Info
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Eras-4001 is a potent, orally active pan- KRAS inhibitor with K d values of 110, 13 and 39 pM against wild-type, G12D and G12V mutant KRAS, respectively, and exhibits selectivity toward wild-type HRAS and NRAS.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3024878-19-8
Sample solution is provided at 25 µL, 10mM.
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In Vivo, Eras-4001 (10-300 mg/kg; p.o.; twice daily for 20 days) exhibits dose-dependent activity in a KRAS G12V non-small cell lung cancer mouse model[1]. Eras-4001 (30-300 mg/kg; p.o.; twice daily for 15 consecutive days) exhibits significant tumor regression in a mouse KRAS G12V ovarian cancer model[1]. Eras-4001 (30-100 mg/kg; p.o.; twice daily for 30 consecutive days) exhibits significant tumor regression in a patient-derived xenograft mouse model of G12D non-small cell lung cancer[1].
In Vitro, Eras-4001 inhibits both active and inactive KRASG12D-RAF1 RBD complex formation with single-digit nanomolar potency[1]. Eras-4001 (3 hours) inhibits ERK phosphorylation in KRASWT and mutant cancer cell lines (AsPC-1, GP2d, MKN1, SW620, RKN, LoVo, LU99, A375), with quantified IC50 values reported[1]. Eras-4001 (4-7 days) potently inhibits 3D cell viability in KRASWT amplified cancer cell lines (IC50 0.7-9.1 nM), KRASG12X mutant cancer cell lines (IC50 0.7-56.0 nM), and KRASG13D mutant cancer cell lines (IC50 0.7-56.0 nM), and has minimal activity in KRASQ61H mutant and KRAS-independent cell lines[1].
References:
[1]. Bae, J. H., et al. (2025). ERAS-4001 is a pan-KRAS inhibitor with robust anti-tumor activity in KRAS altered solid tumors. ERAS, 4001(5.65), 1-65.
| Cas No. | 3024878-19-8 | SDF | |
| Formula | C36H39ClF4N8O3 | M.Wt | 743.19 |
| Solubility | Storage | Store at -20°C | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3456 mL | 6.7278 mL | 13.4555 mL |
| 5 mM | 269.1 μL | 1.3456 mL | 2.6911 mL |
| 10 mM | 134.6 μL | 672.8 μL | 1.3456 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)