Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity.
| Molecular Weight | 1496.65 |
| Formula | C75H101N9O23 |
| CAS Number | 1595275-62-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 200 mg/mL (ultrasonic) |
| Storage | -20°C, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Arnold Lee. Drugs. Loncastuximab Tesirine: First Approval
[3] No authors listed. Am J Health Syst Pharm. Loncastuximab Tesirine-lpyl
| Related Drug-Linker Conjugates for ADC Products |
|---|
| SC-VC-PAB-MMAE
SC-VC-PAB-MMAE is part of a drug-linker conjugate for ADC (ADC) with anticancer activity, which consists of MMAE (a tubulin inhibitor) linked to a cleavable SC-VC-PAB linker. |
| DBCO-(PEG)3-VC-PAB-MMAE
DBCO-(PEG)3-vc-PAB-MMAE is an active molecule coupler (drug-linker conjugate for ADC) consisting of auristatin E attached to a DBCO-(PEG)3-vc-PAB connector. It can be used for cancer research. In addition, DBCO-(PEG)3-vc-PAB-MMAE is a click chemistry that contains a DBCO moiety and can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing an Azide moiety. |
| PB038
PB038 is a drug-liker containing a PEG unit and a cleavable linker attached to Exatecan. |
| Val-Ala-PAB-MMAE
Val-Ala-PAB-MMAE is a Drug-Linker Conjugate for ADC, consisting of ADC linker (Val-Ala-PAB) and MMAE. |
| Val-Ala-PABC-Exatecan
Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor). |
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