DM4-d6 is deuterium labeled DM4. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
786.40
Formula
C38H48D6ClN3O10S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.
Duocarmycin DM free base 是一种 DNA 小沟烷基化剂 (DNA minor-groove alkylator),是一种抗体药物结合物 (ADCs) 毒素。Duocarmycin DM free base 因特有的结构而具有抗癌活性。
Duocarmycin DM free base Chemical Structure
CAS No. : 1116745-06-2
规格
价格
是否有货
数量
5 mg
¥8800
In-stock
10 mg
¥14000
In-stock
25 mg
¥28000
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
Duocarmycin DM free base 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Toxins for Antibody-Drug Conjugate Research Library
生物活性
Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity[1][2].
IC50 & Target[1]
Daunorubicins/Doxorubicins
体外研究 (In Vitro)
The Duocarmycins and CC-1065 are members of a class of DNA minor groove, AT-sequence selective, and adenine-N3 alkylating agents, isolated from Streptomyces sp. that exhibit extremely potent cytotoxicity against the growth of cancer cells grown in culture[2]. Duocarmycin shows cytotoxicity to several human cancer cells, with IC50 of 22, 13.8, 3.87, 15.4, and 7.31 pM for HT-29, CL1-5, Caski, EJ, and LS174T, respectively[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
463.96
Formula
C26H26ClN3O3
CAS 号
1116745-06-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : 50 mg/mL (107.77 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.1554 mL
10.7768 mL
21.5536 mL
5 mM
0.4311 mL
2.1554 mL
4.3107 mL
10 mM
0.2155 mL
1.0777 mL
2.1554 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
参考文献
[1]. Patil PC, et al. A Short Review on the Synthetic Strategies of Duocarmycin Analogs that are Powerful DNA Alkylating Agents. Anticancer Agents Med Chem. 2015;15(5):616-630.
[2]. Koch MF, et al. Structural, Biochemical, and Computational Studies Reveal the Mechanism of Selective Aldehyde Dehydrogenase 1A1 Inhibition by Cytotoxic Duocarmycin Analogues. Angew Chem Int Ed Engl. 2015 Nov 9;54(46):13550-4.
[3]. Chen KC, et al. Selective cancer therapy by extracellular activation of a highly potent glycosidic duocarmycin analogue. Mol Pharm. 2013;10(5):1773-1782.
LDN193189 (DM-3189) is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM)[1].
IC50 & Target[1]
ALK2
5 nM (IC50)
ALK3
30 nM (IC50)
体外研究 (In Vitro)
LDN193189 inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with greater potency than did dorsomorphin (IC50=5 nM versus 470 nM) while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50 for TGF-β ≥1,000 nM). LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase, PDGFR and MAPK signaling pathways as compared to the parent compound. LDN-193189 blocks the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. These findings suggest that LDN193189 might affect BMP-induced osteoblast differentiation. In fact, LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation, indicating sustained BMP signaling activity is needed for osteogenic differentiation[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
In the first experiment, LDN193189 (3 mg/kg) is injected intraperitoneally twice a day after tumors became palpable 7 days post-implantation. The growth rates between the control vehicle- and LDN193189-treated mice are not significantly different after the first 5 weeks, but differences in the growth rates are detected after 6 and 7 weeks post-treatment. In the second experiment, cells are isolated from PCa-118b tumors and injected subcutaneously into SCID mice (1×106 cells per mouse). LDN193189 or vehicle is applied to mice 5 days post-tumor cell injection before tumors are palpable. The differences in the average growth rates between these two groups, as measured by tumor size, are significant at 6 and 7 weeks post-treatment. The tumor weights also show significant differences at the termination of the study at week 7. The X-ray of the tumors shows that the ectopic bone volume and bone density are reduced in the tumors of LDN193189-treated group compared to that of controls[2]. Co-incubation of pulmonary arterial smooth muscle cells (PASMCs) from the pulmonary arterial hypertension (PAH) rats with UK-92480 and LDN193189 completely inhibited the anti-proliferation and up-regulation of the bone morphogenetic protein (BMPR2) and Cx40 expression by the UK-92480[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
406.48
Formula
C25H22N6
CAS 号
1062368-24-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 12 mg/mL (29.52 mM; ultrasonic and adjust pH to 2 with HCl)
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.
[2]. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203.
[3]. Yang L, et al. UK-92480 increases connexin 40 in smooth muscle cells through activation of BMP pathways in pulmonary arterial hypertension. Int J Clin Exp Pathol. 2014 Jul 15;7(8):4674-84.
Cell Assay [1]
Mouse PASMCs grown are transiently transfected to 50% confluence in six-well plates with 0.3 μg Id1promoter luciferase reporter construct (BRE-Luc) in combination with 0.6 μg of plasmid expressing constitutively active forms of BMP type I receptors (caALK2, caALK3 or caALK6). For both reporter plasmids, 0.2 μg of pRL-TKRenilla luciferase are used to control for transfection efficiency. PASMCs are incubated with LDN193189 (2 nM-32 μM) or vehicle starting 1 h after transfection. Cell extracts are harvested and quantified relative promoter activity by the ratio of firefly to Renilla luciferase activity with the dual luciferase assay kit.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2][3]
Mice[2] In the first experiment, SCID mice are implanted with MDA-PCa-118b tumors. After 7 days when tumors reached measurable sizes, mice are injected with LDN193189 (3 mg/kg) or with vehicle intraperitoneally twice a day. Tumor sizes and body weights are measured weekly. Mice are injected with calcein at three days and one day prior to sacrifice. Blood is collected and tumors are weighed. A portion of the tumors are fixed in formaldehyde for micro-computed tomography (microCT), using EVS CT, or further decalcified for bone histomorphometric analysis, using OsteoMeasure Analysis System, or flash frozen for RNA preparation. Osteocalcin in the mouse serum is determined by ELISA. In the second experiment, PCa-118b tumors are first digested with Accumax, and the isolated cells are plated overnight, resuspended in Matrigel in 1:1 ratio, and injected into SCID mice (1×106 cells/mouse) subcutaneously. Mice are treated with LDN193189 five days post-injection. Rats[3] Male Sprague-Dawley (SD) rats, 8 weeks of age, weighing 200-220 g, are purchased from Nanjing Medical University animal center. Rats are randomly assigned to one of seven experiment groups (n=6 per group). Rats are housed with free access to food and water under a natural 12/12 h day/night cycle. The Monocrotaline is administered (60 mg/kg) to rats by subcutaneous injection into the back region. The animal’s lungs are harvested at 28th day of the study after hemodynamic assessment. The UK-92480 group received daily intragastric administration of UK-92480 after the administration of MCT (60 mg/kg). The LDN193189 group received daily intragastric administration of UK-92480 (50 mg/kg) and intraperitoneal injection of LDN193189 (10 mg/kg). In other groups, the same volume saline is given.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.
[2]. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203.
[3]. Yang L, et al. UK-92480 increases connexin 40 in smooth muscle cells through activation of BMP pathways in pulmonary arterial hypertension. Int J Clin Exp Pathol. 2014 Jul 15;7(8):4674-84.
Toxins for Antibody-Drug Conjugate Research Library
Peptidomimetic Library
生物活性
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC)[1][2].
IC50 & Target
Maytansinoids
Clinical Trial
分子量
738.29
Formula
C35H48ClN3O10S
CAS 号
139504-50-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Manu Lopus et al. Maytansine and Cellular Metabolites of Antibody-Maytansinoid Conjugates Strongly Suppress Microtubule Dynamics by Binding to Microtubules.
[2]. Lopus M. Antibody-DM1 conjugates as cancer therapeutics. Cancer Lett. 2011 Aug 28;307(2):113-8.
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis[1][2].
体外研究 (In Vitro)
Ganoderic acid DM (GADM) effectively inhibits cell proliferation and colony formation in MCF-7 human breast cancer cells, which was much stronger than that of MDA-MB-231 breast cancer cells[1]. Ganoderic acid DM especially suppresses the expression of c-Fos and nuclear factor of activated T cells c1 (NFATc1). Ganoderic acid DM markedly suppressed the expression of cathepsin K and TRAP mRNA[2]. Ganoderic acid DM induces autophagic apoptosis in non-small cell lung cancer cells by inhibiting the PI3K/Akt/mTOR activity[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
MCF-7 and MDA-MB-231 cells.
Concentration:
0-100 μM.
Incubation Time:
48 h.
Result:
Decreased the cell viability in breast cancer cells.
Cell Viability Assay[2]
Cell Line:
RAW-D cells.
Concentration:
0-100 μg/mL.
Incubation Time:
0-100 μg/mL.
Result:
Clearly suppressed osteoclastogenesis from the RAW 264 cell D-clone.
分子量
468.67
Formula
C30H44O4
CAS 号
173075-45-1
中文名称
灵芝酸 DM
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Guo-Sheng Wu, et al. Ganoderic acid DM, a natural triterpenoid, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Fitoterapia. 2012 Mar;83(2):408-14.
[2]. Ichiko Miyamoto, et al. Regulation of osteoclastogenesis by ganoderic acid DM isolated from Ganoderma lucidum. Eur J Pharmacol. 2009 Jan 5;602(1):1-7.
[3]. Junbo Xia, et al. Ganoderic acid DM induces autophagic apoptosis in non-small cell lung cancer cells by inhibiting the PI3K/Akt/mTOR activity. Chem Biol Interact. 2020 Jan 25;316:108932.
SMCC-DM1 (DM1-SMCC) is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody drug conjugate (ADC)[1].
IC50 & Target
Maytansinoids
体外研究 (In Vitro)
SMCC-DM1 inhibits HCC1954 and MDA-MB-468 cells proliferation with IC50s of 17.2 and 49.9 nM, respectively[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1072.61
Formula
C51H66ClN5O16S
CAS 号
1228105-51-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Shao S, et al. Site-specific and hydrophilic ADCs through disulfide-bridged linker and branched PEG. Bioorg Med Chem Lett. 2018 May 1;28(8):1363-1370.
Sulfo-PDBA-DM4 is a drug-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker Sulfo-PDBA to make antibody drug conjugate (ADC). Sulfo-PDBA is a gluthatione cleavable linker.
IC50 & Target
Maytansinoids
分子量
978.58
Formula
C42H60ClN3O15S3
CAS 号
1461704-01-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sun X, et al. Effects of Drug-Antibody Ratio on Pharmacokinetics, Biodistribution, Efficacy, and Tolerability of Antibody-Maytansinoid Conjugates. Bioconjug Chem. 2017 May 17;28(5):1371-1381.
DM4-SMCC is a drug-linker conjugate for ADC with antitumor activity by using DM4 (an antitubulin agent), linked via the non-cleavable SMCC linker[1].
IC50 & Target
Maytansinoids
分子量
1114.69
Formula
C54H72ClN5O16S
CAS 号
1228105-52-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Singh R, et al. A New Triglycyl Peptide Linker for Antibody-Drug Conjugates (ADCs) with Improved TargetedKilling of Cancer Cells. Mol Cancer Ther. 2016 Jun;15(6):1311-20.
SPP-DM1 is a drug-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker SPP[1].
IC50 & Target
Maytansinoids
分子量
967.54
Formula
C44H59ClN4O14S2
CAS 号
452072-20-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Manu Lopus et al. Maytansine and Cellular Metabolites of Antibody-Maytansinoid Conjugates Strongly Suppress Microtubule Dynamics by Binding to Microtubules.
S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects[1][2].
IC50 & Target
Maytansinoids
体外研究 (In Vitro)
S-methyl DM1 is the primary cellular or liver metabolite of antibody-maytansinoid conjugates prepared with thiol-containing maytansinoids DM1[1]. The half-maximal concentration for inhibition of microtubule assembly for for S-methyl DM1 is 4 μM. At 100 nM S-methyl-DM1 (84%) suppresses dynamic instability more strongly than Maytansine (45%). Tritiated S-methyl-DM1 bound to 37 high-affinity sites per microtubule (Kd of 0.1 μM)[1]. The concentration dependence curves for the inhibition of cell proliferation by S-methyl DM1 is sigmoidal in shape in MCF7 cells. Minimal inhibition occurred at 200 pM S-methyl DM1, and inhibition is maximal at 3 nM. S-methyl DM1 (IC50 of 330 pM) is slightly more potent than Maytansine (IC50 of 710 pM)[2]. S-methyl DM1 induces maxima of 80% accumulation of cells in G2/M as compared with only 30% in controls in MCF7 cells[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
752.31
Formula
C36H50ClN3O10S
CAS 号
912569-84-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Lopus M, et al. Maytansine and cellular metabolites of antibody-maytansinoid conjugates strongly suppress microtubule dynamics by binding to microtubules. Mol Cancer Ther. 2010 Oct;9(10):2689-99.
[2]. Oroudjev E, et al. Maytansinoid-antibody conjugates induce mitotic arrest by suppressing microtubule dynamic instability. Mol Cancer Ther. 2010 Oct;9(10):2700-13.
DM3-SMe is a maytansine derivative and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM3-SMe shows highly cytotoxic activity in vitro with an IC50 of 0.0011 nM[1][2].
IC50 & Target[1]
Maytansinoids
分子量
812.43
Formula
C38H54ClN3O10S2
CAS 号
796073-70-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Chen H, et al. Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy. Molecules. 2017 Aug 1;22(8).
DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate[1]. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].
IC50 & Target[1]
Maytansinoids
分子量
981.57
Formula
C45H61ClN4O14S2
CAS 号
2245698-48-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.
[2]. Lobedanz S et al. A periplasmic coiled-coil interface underlying TolC recruitment and the assembly of bacterial drug effluxpumps. Proc Natl Acad Sci U S A, 2007 Mar 13, 104(11):4612-7.
[3]. Karumuthil-Melethil S et al. Dendritic cell-directed CTLA-4 engagement during pancreatic beta cell antigen presentation delays type 1diabetes. J Immunol 2010 Jun 15, 184(12):6695-708.
DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs)[1].
IC50 & Target
Maytansinoids
分子量
766.34
Formula
C37H52ClN3O10S
CAS 号
796073-54-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Chen H, et al. Tubulin Inhibitor-Based Antibody-Drug Conjugates for Cancer Therapy. Molecules. 2017 Aug 1;22(8).
Toxins for Antibody-Drug Conjugate Research Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Covalent Screening Library
Cytoskeleton Compound Library
Anti-Lung Cancer Compound Library
生物活性
DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
体外研究 (In Vitro)
DM4, a structural analogue of maytansine, is a new thiol-containing and potent maytansinoid. DM4 is a cytotoxic maytansinoid drug. It is synthesized in order to link maytansinoids to antibodies via disulfide bonds. Maytansinoids inhibit tubulin polymerization and microtubule assembly and enhance microtubule destabilization, so there is potent suppression of microtubule dynamics resulting in a mitotic block and subsequent apoptotic cell death[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
780.37
Formula
C38H54ClN3O10S
CAS 号
796073-69-3
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tang R, et al. P-gp activity is a critical resistance factor against AVE9633 and DM4 cytotoxicity in leukaemia cell lines, but not a major mechanism of chemoresistance in cells from acute myeloid leukaemia patients. BMC Cancer. 2009 Jun 23;9:199.
Duocarmycin DM, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity[1][2].
IC50 & Target
Daunorubicins/Doxorubicins
体外研究 (In Vitro)
The Duocarmycins and CC-1065 are members of a class of DNA minor groove, AT-sequence selective, and adenine-N3 alkylating agents, isolated from Streptomyces sp. that exhibit extremely potent cytotoxicity against the growth of cancer cells grown in culture[2]. Duocarmycin DM shows cytotoxicity to several human cancer cells, with IC50 of 22, 13.8, 3.87, 15.4, and 7.31 pM for HT-29, CL1-5, Caski, EJ, and LS174T, respectively[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
577.98
Formula
C28H27ClF3N3O5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Patil PC, et al. A Short Review on the Synthetic Strategies of Duocarmycin Analogs that are Powerful DNA Alkylating Agents. Anticancer Agents Med Chem. 2015;15(5):616-630.
[2]. Koch MF, et al. Structural, Biochemical, and Computational Studies Reveal the Mechanism of Selective Aldehyde Dehydrogenase 1A1 Inhibition by Cytotoxic Duocarmycin Analogues. Angew Chem Int Ed Engl. 2015 Nov 9;54(46):13550-4.
[3]. Chen KC, et al. Selective cancer therapy by extracellular activation of a highly potent glycosidic duocarmycin analogue. Mol Pharm. 2013;10(5):1773-1782.
DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody drug conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
IC50 & Target
Maytansinoids
分子量
1297.92
Formula
C68H89ClN6O17
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
IC50 & Target
Maytansinoids
分子量
995.59
Formula
C46H63ClN4O14S2
CAS 号
1626359-62-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-80°C, protect from light, stored under nitrogen
溶解性数据
In Vitro:
DMSO : 50 mg/mL (50.22 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.0044 mL
5.0221 mL
10.0443 mL
5 mM
0.2009 mL
1.0044 mL
2.0089 mL
10 mM
0.1004 mL
0.5022 mL
1.0044 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: