Deruxtecan
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $2500 | Check With Us |
| 1g | $4000 | Check With Us |
: Cat #: V4653 CAS #: 1599440-13-7 Purity ≥ 95%
Description: Deruxtecan (DS-8201a; DS8201a; exatecan analog; DX-8951 analog), a drug-linker conjugate for antibody-drug conjugate (ADC, Patritumab deruxtecan or U3-1402), is a novel, potent toxin and linker moiety of DS-8201.
References: [1]. NOGUCHI, Shigeru, et al. METHOD FOR SELECTIVELY MANUFACTURING ANTIBODY-DRUG CONJUGATE. WO2017002776A1.
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| Molecular Weight (MW) | 1034.05 |
|---|---|
| Molecular Formula | C52H56FN9O13 |
| CAS No. | 1599440-13-7 |
| Storage | -20℃ for 3 years in powder formrrrrrrrr |
| -80℃ for 2 years in solvent | |
| SMILES Code | CC[C@@]1(O)C(OCC2=C1C=C3N(C2=O)CC(C3=NC4=CC(F)=C5C)=C6C4=C5CC[C@@H]6NC(COCNC(CNC([C@@H](NC(CNC(CNC(CCCCCN7C(C=CC7=O)=O)=O)=O)=O)CC8=CC=CC=C8)=O)=O)=O)=O |
| Synonyms | Deruxtecan; DS-8201a; DS 8201a; DS8201a; exatecan derivative; DX 8951; DX8951; DX-8951 derivative; Trastuzumab deruxtecan; |
| Protocol | In Vitro | Antibody-drug conjugates deliver anticancer agents selectively and efficiently to tumor tissue and have significant antitumor efficacy with a wide therapeutic window[2]. The antitumor activity of [fam-] trastuzumab deruxtecan for CRC with five CRC cell lines that possess different biological characteristics was investigated. The expression of HER2 at both mRNA and protein levels in these various cell lines was first examined. Immunoblot analysis and RT and real-time polymerase chain reaction (PCR) analysis revealed that the amounts of HER2 protein and HER2 mRNA were much smaller in all the CRC cell lines than in NCI-N87 cells. [fam-] trastuzumab deruxtecan attenuated the viability of NCI-N87 cells, consistent with previous results, whereas all five CRC cell lines showed resistance to this agent. These findings suggested that the expression level of HER2 protein might determine sensitivity to [fam-] trastuzumab deruxtecan |
|---|---|---|
| In Vivo | The efficacy of [fam-] trastuzumab deruxtecan in HER2-expressing xenograft tumor models was tested. It was first confirmed that HER2 protein expression levels by immunohistochemistry (IHC) in subcutaneous tumors formed in nude mice by HCT116-Mock, HCT116-H2L or HCT116-H2H cells. Administration of [fam-] trastuzumab deruxtecan at a dose of 3.0 mg/kg markedly inhibited the growth of tumors formed by HCT116-H2L or HCT116-H2H cells but not that of those formed by HCT116-Mock cells. The extents of the inhibition by [fam-] trastuzumab deruxtecan were 60 and 93% compared to PBS vehicle for HCT116-H2L and HCT116-H2H cells, respectively, on day 24. Treatment with [fam-] trastuzumab deruxtecan had no effect on body weight in any of the three groups of mice. These findings thus indicated that the sensitivity of tumors to [fam-] trastuzumab deruxtecan in xenograft models is dependent on HER2 expression level and that such treatment is not associated with overt toxicity. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 0.9671 mL | 4.8354 mL | 9.6707 mL | 19.3414 mL |
| 5mM | 0.1934 mL | 0.9671 mL | 1.9341 mL | 3.8683 mL |
| 10mM | 0.0967 mL | 0.4835 mL | 0.9671 mL | 1.9341 mL |
| 20mM | 0.0484 mL | 0.2418 mL | 0.4835 mL | 0.9671 mL |
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