There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Mertansine (DM1) serves as a microtubulin inhibitor and is a maytansinoid designed for conjugation to antibodies to form antibody-drug conjugates (ADCs), aimed at reducing systemic toxicity associated with maytansine and improving tumor-specific delivery[1].[2].
体内研究
Despite its efficacy, mertansine has a relatively low maximum-tolerated dose (MTD) of 1 mg/kg[3].
体外研究
Mertansine demonstrates potent antiproliferative effects against over 60 types of cancer cell lines, showcasing broad chemotherapeutic potential[3].
Mertansine exhibits antitumor activity against malignant B16F10 melanoma cells, particularly when combined with DTX, by inhibiting tumor cell growth through the disruption of mitosis[3].
DM1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human hepatocytes
1.25–2500 nM
48 hours
To evaluate the inhibitory effects of mertansine on mRNA expression of CYP1A2, CYP2B6, CYP3A4, CYP2C8, CYP2C9, CYP2C19, UGT1A1, UGT1A4, and UGT1A9. Results showed that mertansine dose-dependently suppressed the mRNA levels of these enzymes.
Pharmaceutics. 2020 Mar 2;12(3):220.
Human liver microsomes
0.01–50 µM
60 minutes
To evaluate the inhibitory effects of mertansine on UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, and UGT2B7 enzyme activities. Results showed that mertansine inhibited UGT1A1, UGT1A3, and UGT1A4 activities but had no effect on UGT1A6, UGT1A9, and UGT2B7.
Pharmaceutics. 2020 Mar 2;12(3):220.
EL-4 WT cells
1.71 nM to 416 nM
72 hours
To evaluate the cytotoxic effect of VHH A1-DM1 on WT cells, results showed no obvious cytotoxicity on WT cells.
Front Immunol. 2024 Mar 14;15:1368586.
EL-4 MICA+ cells
1.71 nM to 416 nM
72 hours
To evaluate the cytotoxic effect of VHH A1-DM1 on MICA+ cells, results showed that VHH A1-DM1 had a strong cytotoxic effect on MICA+ cells at low doses, with an IC50 comparable to free DM4.
Front Immunol. 2024 Mar 14;15:1368586.
DM1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
A549 tumor xenograft model
Intravenous injection
0.8 mg/kg
Recorded every 2 days for 15 days
To evaluate the in vivo antitumor efficacy of DM1-loaded ZNPs, results showed a tumor inhibition rate of 97.3%, superior to free DM1's 92.7%.
Drug Deliv. 2020 Dec;27(1):100-109.
C57BL/6 mice
B16-F10 melanoma model
Intraperitoneal injection
20 nmol/kg
Every 3 days for a total of 5 times
To evaluate the therapeutic effects of M-DM1 in a Mice model of melanoma. Results showed that M-DM1 significantly suppressed tumor growth, prolonged survival, and enhanced the infiltration of CD8+ cytotoxic T cells and NK cells in the tumor microenvironment.
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