VcMMAE is a MMAE derivative with valine-citrulline (Vc) linker. Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells. MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. In vivo, Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models.
*The compound is unstable in solutions, freshly prepared is recommended
Molecular Weight | 1316.63 |
Formula | C68H105N11O15 |
CAS Number | 646502-53-6 |
Solubility (25°C) | DMSO: ≥ 42 mg/mL |
Storage | 4°C, protect from light, dry, 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.
Related Microtubule Products |
---|
P34cdc2 Kinase Fragment
P34cdc2 Kinase Fragment is associated with the completion of DNA replication in yeast mitosis. |
Cemadotin
Cemadotin (LU103793) is an analogue of Dolastatin 15 which is naturally occurring cytotoxic peptides. |
VLS-1488
VLS-1488 is an orally active KIF18A inhibitor that inhibits KIF18A microtubule-dependent ATPase activity with an IC50 value of 0.016 μM. |
ENMD-1198
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. |
Tubulin/JAK2-IN-1
Tubulin/JAK2-IN-1 is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.