MCC-DM1

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the clinical use of trastuzumab emtansine during breastfeeding. Because trastuzumab is a large protein molecule with a molecular weight of 145,531 Da, the amount in milk is likely to be very low. It is also likely to be partially destroyed in the infant's gastrointestinal tract and absorption by the infant is probably minimal. However, emtansine (DM1) is a small-molecule microtubule inhibitory drug, which might be excreted into milk. The manufacturer recommends that breastfeeding be discontinued during trastuzumab deruxtecan therapy and for 7 months after the last dose.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
◉ Summary of Use during Lactation
No information is available on the clinical use of ado-trastuzumab during breastfeeding. Because trastuzumab is a large protein molecule with a molecular weight of 145,531 Da, the amount in milk is likely to be very low. It is also likely to be partially destroyed in the infant's gastrointestinal tract and absorption by the infant is probably minimal. However, ado-trastuzumab emtansine also contains DM1, which is a small-molecule toxin that might enter milk and be absorbed by the infant. Because of the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends avoiding breastfeeding during and for 7 months following ado-trastuzumab emtansine therapy.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[1]. Antibody-DM1 conjugates as cancer therapeutics. Cancer Lett. 2011 Aug 28;307(2):113-8.

[2]. LC-MS/MS method for the simultaneous determination of Lys-MCC-DM1, MCC-DM1 and DM1 as potential intracellular catabolites of the antibody-drug conjugate trastuzumab emtansine (T-DM1). J Pharm Biomed Anal. 2017 Apr 15;137:170-177.

Immunotoxin that consists of humanized monoclonal anti-HER2 antibody TRASTUZUMAB covalently linked to anti-microtubule agent MAYTANSINOID DM1 for treatment of metastatic breast cancer in patients who previously received trastuzumab and a TAXANES, separately or in combination.
See also: Trastuzumab Emtansine (annotation moved to).

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Drug Indication
Early Breast Cancer (EBC)Kadcyla, as a single agent, is indicated for the adjuvant treatment of adult patients with HER2-positive early breast cancer who have residual invasive disease, in the breast and/or lymph nodes, after neoadjuvant taxane-based and HER2-targeted therapy. Metastatic Breast Cancer (MBC)Kadcyla, as a single agent, is indicated for the treatment of adult patients with HER2-positive, unresectable locally advanced or metastatic breast cancer who previously received trastuzumab and a taxane, separately or in combination. Patients should have either: Received prior therapy for locally advanced or metastatic disease, orDeveloped disease recurrence during or within six months of completing adjuvant therapy.

C47H64CLN5O13S

974.55

973.39

1100692-14-5

166596981

White to off-white solid powder

2

262

3

14

13

67

1950

8

C[C@]12[C@]([H])(CC(N(C3=C(C(OC)=CC(CC(C)=CC=C[C@@]([H])(OC)[C@@]4(NC(=O)O[C@@]([H])(C4)[C@@H](C)[C@@H]1O2)O)=C3)Cl)C)=O)OC(=O)[C@H](C)N(C)C(=O)CCSC1CC(=O)N(CC2CCC(C(=O)N)CC2)C1=O |t:16,18,&1:1,2,20,24,29,32,34,44|

WPWQMVXPTHKASL-KLVLVJRKSA-N

InChI=1S/C47H64ClN5O13S/c1-25-10-9-11-35(63-8)47(61)23-33(64-45(60)50-47)26(2)41-46(4,66-41)36(22-38(55)52(6)31-19-29(18-25)20-32(62-7)40(31)48)65-44(59)27(3)51(5)37(54)16-17-67-34-21-39(56)53(43(34)58)24-28-12-14-30(15-13-28)42(49)57/h9-11,19-20,26-28,30,33-36,41,61H,12-18,21-24H2,1-8H3,(H2,49,57)(H,50,60)/b11-9-,25-10-/t26-,27+,28?,30?,33+,34?,35-,36+,41+,46+,47+/m1/s1

[(1S,2R,3S,5S,6S,16Z,18Z,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[1-[(4-carbamoylcyclohexyl)methyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoyl-methylamino]propanoate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : 190 mg/mL (194.96 mM)

配方 1 中的溶解度: ≥ 4.75 mg/mL (4.87 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 47.5 mg/mL澄清的DMSO储备液加入到400 μL PEG300中，混匀；再向上述溶液中加入50 μL Tween-80，混匀；然后加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 4.75 mg/mL (4.87 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 47.5mg/mL澄清的DMSO储备液加入到900μL 20％SBE-β-CD生理盐水中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 4.75 mg/mL (4.87 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 47.5 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。