WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408188
CAS#: 1375089-56-7
Description: MC-DM is a Maytansine derative and a DM1 molecule with an reactive linker MC. MC-DM1 is a useful precursor to make drug antibody congjuate (ADC) such as HER2-Targeting Affibody-DM1 Drug Conjugates. The resulting affibody drug conjugates were potent cytotoxic molecules for human cells over-expressing HER2, with sub-nanomolar IC50-values similar to trastuzumab emtansine, and did not affect cells with low HER2 expression. A biodistribution study of a radiolabeled version of (ZHER2:2891)2-ABD-MC-DM1, showed that it was taken up by the tumor. The major site of off-target uptake was the kidneys and to some extent the liver. (ZHER2:2891)2-ABD-MC-DM1 was found to have a half-life in circulation of 14 h. The compound was tolerated well by mice at 8.5 mg/kg and was shown to extend survival of mice bearing HER2 over-expressing tumors.
MedKoo Cat#: 408188
Name: MC-DM1
CAS#: 1375089-56-7
Chemical Formula: C42H55ClN4O12
Exact Mass: 842.3505
Molecular Weight: 843.368
Elemental Analysis: C, 59.82; H, 6.57; Cl, 4.20; N, 6.64; O, 22.76
Synonym: MC-DM1; MC DM1; MCDM1; Maytansine, N2′-deacetyl-N2′-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-;
IUPAC/Chemical Name: (14S,16S,32S,33S,2R,4S,10E,12E,14R)-86-chloro-14-hydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-12,6-dioxo-7-aza-1(6,4)-oxazinana-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-4-yl N-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl)-N-methyl-L-alaninate
InChi Key: GBPANNIQRLRII-RJPAQOSPSA-N
InChi Code: InChI=1S/C42H55ClN4O12/c1-24-13-12-14-31(56-8)42(54)23-30(57-40(53)44-42)25(2)38-41(4,59-38)32(22-36(51)46(6)28-20-27(19-24)21-29(55-7)37(28)43)58-39(52)26(3)45(5)33(48)15-10-9-11-18-47-34(49)16-17-35(47)50/h12-14,16-17,20-21,25-26,30-32,38,54H,9-11,15,18-19,22-23H2,1-8H3,(H,44,53)/b14-12+,24-13+/t25-,26+,30+,31-,32+,38+,41+,42+/m1/s1
SMILES Code: C[C@]12[C@@](O1)([C@H](C)[C@@]3(C[C@](O)([C@H](OC)/C=C/C=C(\C)/CC4=CC(N(C)C(=O)C[C@@H]2OC([C@@H](N(C(CCCCCN5C(=O)C=CC5=O)=O)C)C)=O)=C(Cl)C(OC)=C4)NC(=O)O3)[H])[H]
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 843.368 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Ding H, Altai M, Rinne SS, Vorobyeva A, Tolmachev V, Gräslund T, Orlova A. Incorporation of a Hydrophilic Spacer Reduces Hepatic Uptake of HER2-Targeting Affibody-DM1 Drug Conjugates. Cancers (Basel). 2019 Aug 14;11(8):1168. doi: 10.3390/cancers11081168. PMID: 31416167; PMCID: PMC6721809.
2: Altai M, Liu H, Ding H, Mitran B, Edqvist PH, Tolmachev V, Orlova A, Gräslund T. Affibody-derived drug conjugates: Potent cytotoxic molecules for treatment of HER2 over-expressing tumors. J Control Release. 2018 Oct 28;288:84-95. doi: 10.1016/j.jconrel.2018.08.040. Epub 2018 Aug 30. PMID: 30172673.
