購物車 
-
DC41SMe
- names：
DC41SMe
- CAS號：
1354787-71-5
MDL Number： No data available - MF(分子式)： C38H36ClN5O4S2 MW(分子量)： 726.31
- EINECS:No data available Reaxys Number:No data available
- Pubchem ID:No data available Brand:BIOFOUNT
DC41SMe(1354787-71-5)是DC1衍生物，在Ramos，Namalwa和HL60 / s細胞中表現(xiàn)出細胞毒性，IC50范圍為18-25 pM。 DC1是CC-1065的簡化類似物，是細胞毒性DNA烷基化劑的抗體偶聯(lián)物，用于靶向治療癌癥。
| 貨品編碼 | 規(guī)格 | 純度 | 價格 (￥) | 現(xiàn)價(￥) | 特價(￥) | 庫存描述 | 數(shù)量 | 總計 (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000924-250mg | 250mg | >95% | ￥ 0.00 | ￥ 0.00 | Backorder | ￥ 0.00 | ||
| YZM000924-100mg | 100mg | >95% | ￥ 0.00 | ￥ 0.00 | Backorder | ￥ 0.00 |
| 中文別名 | DC41SMe(1354787-71-5) |
| 英文別名 | DC41SMe,1354787-71-5 |
| CAS號 | 1354787-71-5 |
| Inchi | No data available |
| InchiKey | No data available |
| 分子式 Formula | C38H36ClN5O4S2 |
| 分子量 Molecular Weight | 726.31 |
| 溶解度Solubility | |
| 性狀 | Solid |
| 儲藏條件 Storage conditions | 請根據(jù)產(chǎn)品建議的存儲條件進行存儲,Please store the product under the recommended condition sin the description. |
DC41SMe(1354787-71-5)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染
DC41SMe(1354787-71-5) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
Tag:DC41SMe(1354787-71-5),DC41SMe試劑,DC41SMe抑制劑,DC41SMe的純度,DC41SMe的作用,DC41SMe的使用,DC41SMe的合成,DC41SMe的MSDS,DC41SMe的COA,DC41SMe的生產(chǎn),DC41SMe的效果,DC41SMe的注意事項,DC41SMe的外觀,DC41SMe的溶解度
| 產(chǎn)品說明 | DC41SMe(1354787-71-5)是一種有效的 DC1 衍生物，對 Ramos、Namalwa 和 HL60/s 細胞顯示細胞毒性. |
| Introduction | DC41SMe(1354787-71-5), a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC50s ranging from 18-25 pM. |
| Application1 | |
| Application2 | |
| Application3 |
1.Antibody-drug conjugates designed to eradicate tumors with homogeneous and heterogeneous expression of the target antigen
Kovtun YV, Audette CA, Ye Y, Xie H, Ruberti MF, Phinney SJ, Leece BA, Chittenden T, Blättler WA, Goldmacher VS.
Conjugates of the anti-CanAg humanized monoclonal antibody huC242 with the microtubule-formation inhibitor DM1 (a maytansinoid), or with the DNA alkylator DC1 (a CC1065 analogue), have been evaluated for their ability to eradicate mixed cell populations formed from CanAg-positive and CanAg-negative cells in culture and in xenograft tumors in mice. We found that in culture, conjugates of either drug killed not only the target antigen-positive cells but also the neighboring antigen-negative cells. Furthermore, we showed that, in vivo, these conjugates were effective in eradicating tumors containing both antigen-positive and antigen-negative cells. The presence of antigen-positive cells was required for this killing of bystander cells. This target cell-activated killing of bystander cells was dependent on the nature of the linker between the antibody and the drug. Conjugates linked via a reducible disulfide bond were capable of exerting the bystander effect whereas equally potent conjugates linked via a nonreducible thioether bond were not. Our data offer a rationale for developing optimally constructed antibody-drug conjugates for treating tumors that express the target antigen either in a homogeneous or heterogeneous manner.
Kovtun YV, Audette CA, Ye Y, Xie H, Ruberti MF, Phinney SJ, Leece BA, Chittenden T, Blättler WA, Goldmacher VS.
Conjugates of the anti-CanAg humanized monoclonal antibody huC242 with the microtubule-formation inhibitor DM1 (a maytansinoid), or with the DNA alkylator DC1 (a CC1065 analogue), have been evaluated for their ability to eradicate mixed cell populations formed from CanAg-positive and CanAg-negative cells in culture and in xenograft tumors in mice. We found that in culture, conjugates of either drug killed not only the target antigen-positive cells but also the neighboring antigen-negative cells. Furthermore, we showed that, in vivo, these conjugates were effective in eradicating tumors containing both antigen-positive and antigen-negative cells. The presence of antigen-positive cells was required for this killing of bystander cells. This target cell-activated killing of bystander cells was dependent on the nature of the linker between the antibody and the drug. Conjugates linked via a reducible disulfide bond were capable of exerting the bystander effect whereas equally potent conjugates linked via a nonreducible thioether bond were not. Our data offer a rationale for developing optimally constructed antibody-drug conjugates for treating tumors that express the target antigen either in a homogeneous or heterogeneous manner.
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
Synthesis and biological evaluation of antibody conjugates of phosphate prodrugs of cytotoxic DNA alkylators for the targeted treatment of cancer
Zhao RY, Erickson HK, Leece BA, Reid EE, Goldmacher VS, Lambert JM, Chari RV.
The synthesis and biological evaluation of phosphate prodrugs of analogues of 1 (CC-1065) and their conjugates with antibodies are described. The phosphate group on the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) portion of the compounds confers enhanced solubility and stability in aqueous solutions. In the presence of phosphatases, these compounds convert into active DNA-alkylating agents. The synthesis of the prodrugs was achieved sequentially through coupling of CBI with a bis-indolyl moiety, followed by attachment of a thiol-containing linker, and conversion of the hydroxyl group of CBI into a phosphate prodrug. The linkers incorporated into the prodrugs enable conjugation to an antibody via either a stable disulfide or thioether bond, in aqueous buffer solutions containing as little as 5% organic cosolvent, resulting in exclusively monomeric and stable antibody-cytotoxic prodrug conjugates. Two disulfide-containing linkers differing in the degree of steric hindrance were used in antibody conjugates to test the effect of different rates of intracellular disulfide cleavage and effector release on biological activity. The prodrugs can be converted to the active cytotoxic compounds through the action of endogenous phosphatases. Antibody-prodrug conjugates displayed potent antigen-selective cytotoxic activity in vitro and antitumor activity in vivo.
Zhao RY, Erickson HK, Leece BA, Reid EE, Goldmacher VS, Lambert JM, Chari RV.
The synthesis and biological evaluation of phosphate prodrugs of analogues of 1 (CC-1065) and their conjugates with antibodies are described. The phosphate group on the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) portion of the compounds confers enhanced solubility and stability in aqueous solutions. In the presence of phosphatases, these compounds convert into active DNA-alkylating agents. The synthesis of the prodrugs was achieved sequentially through coupling of CBI with a bis-indolyl moiety, followed by attachment of a thiol-containing linker, and conversion of the hydroxyl group of CBI into a phosphate prodrug. The linkers incorporated into the prodrugs enable conjugation to an antibody via either a stable disulfide or thioether bond, in aqueous buffer solutions containing as little as 5% organic cosolvent, resulting in exclusively monomeric and stable antibody-cytotoxic prodrug conjugates. Two disulfide-containing linkers differing in the degree of steric hindrance were used in antibody conjugates to test the effect of different rates of intracellular disulfide cleavage and effector release on biological activity. The prodrugs can be converted to the active cytotoxic compounds through the action of endogenous phosphatases. Antibody-prodrug conjugates displayed potent antigen-selective cytotoxic activity in vitro and antitumor activity in vivo.
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