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Cayman Epertinib (hydrochloride), 1 mg


Product Description
Epertinib is an inhibitor of EGFR, HER2, and HER4 (IC50s = 1.48, 7.15, and 2.49 nM, respectively).1 It is selective for these kinases over VEGFR2, insulin-like growth factor 1 receptor (IGF-1R), c-Src, KIT, and PDGFRβ (IC50s = >10,000 nM for all). Epertinib inhibits EGFR and HER2 autophosphorylation in NCI N87 gastric carcinoma cells (IC50s = 4.5 and 1.6 nM, respectively). It selectively inhibits the growth of NCI N87, BT474 breast, and HT115 colon carcinoma cancer cell lines (IC50s = 8.3, 9.9, and 53.3 nM, respectively) over fR2 breast epithelial cells and MRC-5 fibroblasts (IC50s = 5,366.7 and 4,964.6 nM, respectively). Epertinib (12.5 or 50 mg/kg per day) decreases tumor volume in an NCI N87 mouse xenograft model.
WARNING This product is not for human or veterinary use.
Technical Information
| Formal Name | 1-[4-[[3- |
| CAS Number | 2071195-74-7 |
| Synonyms |
|
| Molecular Formula | C30H27ClFN5O3 • HCl |
| Formula Weight | 596.5 |
| Purity | ≥98% |
| Formulation(Request formulation change) | A solid |
| Solubility(Learn about Variance in Solubility) | DMSO: Soluble: ≥10 mg/mL |
| SMILES | FC1=CC=CC(COC(C=CC(NC2=NC=NC3=C2C=C(C=C3)/C(C#CC)=N/OC[C@@H]4NCCOC4)=C5)=C5Cl)=C1.Cl |
| InChi Code | InChI=1S/C30H27ClFN5O3.ClH/c1-2-4-27(37-40-18-24-17-38-12-11-33-24)21-7-9-28-25(14-21)30(35-19-34-28)36-23-8-10-29(26(31)15-23)39-16-20-5-3-6-22(32)13-20;/h3,5-10,13-15,19,24,33H,11-12,16-18H2,1H3,(H,34,35,36);1H/b37-27+;/t24-;/m1./s1 |
| InChi Key | NVWJPQQXBPWOOA-PLXRJBJVSA-N |
Shipping & Storage Information
| Storage | -20°C |
| Shipping | Room temperature in continental US; may vary elsewhere |
| Stability | ≥ 4 years |
| SKU | CAYM-44442-1 |
|---|---|
| Supplier Part Number | 44442-1 |
| UM | EA |
| UNSPSC | 12352200 |
| Manufacturer | Cayman |
| Temperature | -20 |
| Refrigerated-Frozen | Y |
| CountryOfOrigin | China |
| ProductLine | CAYM |
| Qty | 1 |
| MinOrderQty | 1 |
| Weight | 7.000000 |
| Lead Time | 5 |
| Hazardous | N |
| CAS Number | 2071195-74-7 |
| Energy Star | No |
| Green | No |
| Controlled | N |

