Val-Cit-PAB-MMAE
Val-Cit-PAB-MMAE is a MMAE derivative with a cleavable linker, which is useful to make MMAE conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE. MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
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Chemical Information
| Name | Val-Cit-PAB-MMAE |
|---|---|
| Iupac Chemical Name | 4-((S)-2-((S)-2-amino-3-methylbutanamido)-5-ureidopentanamido)benzyl ((S)-1-(((S)-1-(((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)(methyl)amino)-3-methyl-1-oxobutan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)(methyl)carbamate |
| Synonyms | Val-Cit-PAB-MMAE; MMAE ADC conjugate; |
| Molecular Formula | C58H94N10O12 |
| Molecular Weight | 1123.448 |
| Smile | CC[C@H](C)[C@@H]([C@@H](CC(N1[C@@H](CCC1)[C@@H]([C@@H](C)C(N[C@H](C)[C@@H](O)C2=CC=CC=C2)=O)OC)=O)OC)N(C([C@H](C(C)C)NC([C@H](C(C)C)N(C(OCC3=CC=C(NC([C@H](CCCNC(N)=O)NC([C@H](C(C)C)N)=O)=O)C=C3)=O)C)=O)=O)C |
| InChiKey | WZEAGSMYTVSXQA-XZZQEHRXSA-N |
| InChi | InChI=1S/C58H94N10O12/c1-15-36(8)49(44(78-13)31-45(69)68-30-20-24-43(68)51(79-14)37(9)52(71)62-38(10)50(70)40-21-17-16-18-22-40)66(11)56(75)47(34(4)5)65-55(74)48(35(6)7)67(12)58(77)80-32-39-25-27-41(28-26-39)63-53(72)42(23-19-29-61-57(60)76)64-54(73)46(59)33(2)3/h16-18,21-22,25-28,33-38,42-44,46-51,70H,15,19-20,23-24,29-32,59H2,1-14H3,(H,62,71)(H,63,72)(H,64,73)(H,65,74)(H3,60,61,76)/t36-,37+,38+,42-,43-,44+,46-,47-,48-,49-,50+,51+/m0/s1 |
| CAS Number | 644981-35-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| 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. |
| HS Code |
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| Mechanism | |
| Cell study | |
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| Clinical study |
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4: Amatore F, Ortonne N, Lopez M, Orlanducci F, Castellano R, Ingen-Housz-Oro S, De Croos A, Salvado C, Gorvel L, Goubard A, Collette Y, Bouabdallah R, Schiano JM, Bonnet N, Grob JJ, Gaulard P, Bagot M, Bensussan A, Berbis P, Olive D. ICOS is widely expressed in cutaneous T-cell lymphoma, and its targeting promotes potent killing of malignant cells. Blood Adv. 2020 Oct 27;4(20):5203-5214. doi: 10.1182/bloodadvances.2020002395. PMID: 33095875; PMCID: PMC7594390.
5: Pan D, Tang Y, Tong J, Xie C, Chen J, Feng C, Hwu P, Huang W, Zhou D. An antibody-drug conjugate targeting a GSTA glycosite-signature epitope of MUC1 expressed by non-small cell lung cancer. Cancer Med. 2020 Oct 20. doi: 10.1002/cam4.3554. Epub ahead of print. PMID: 33084221.
6: Jendryczko K, Chudzian J, Skinder N, Opaliński Ł, Rzeszótko J, Wiedlocha A, Otlewski J, Szlachcic A. FGF2-Derived PeptibodyF2-MMAE Conjugate for Targeted Delivery of Cytotoxic Drugs into Cancer Cells Overexpressing FGFR1. Cancers (Basel). 2020 Oct 15;12(10):2992. doi: 10.3390/cancers12102992. PMID: 33076489; PMCID: PMC7602595.
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12: Jin R, Liu L, Xing Y, Meng T, Ma L, Pei J, Cong Y, Zhang X, Ren Z, Wang X, Shen J, Yu K. Dual Mechanisms of Novel CD73-Targeted Antibody and Antibody-Drug Conjugate in Inhibiting Lung Tumor Growth and Promoting Antitumor Immune- Effector Function. Mol Cancer Ther. 2020 Sep 17. doi: 10.1158/1535-7163.MCT-20-0076. Epub ahead of print. PMID: 32943546.
13: Wang S, Wen H, Fei W, Zhao Y, Feng Y, Kuang L, Wang M, Wu M. Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. PMID: 32905508; PMCID: PMC7471348.
14: Yaghoubi S, Gharibi T, Karimi MH, Sadeqi Nezhad M, Seifalian A, Tavakkol R, Bagheri N, Dezhkam A, Abdollahpour-Alitappeh M. Development and biological assessment of MMAE-trastuzumab antibody-drug conjugates (ADCs). Breast Cancer. 2020 Sep 5. doi: 10.1007/s12282-020-01153-5. Epub ahead of print. PMID: 32889587.
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19: Lu T, Gibiansky L, Li X, Li C, Shi R, Agarwal P, Hirata J, Miles D, Chanu P, Girish S, Jin JY, Lu D. Exposure-safety and exposure-efficacy analyses of polatuzumab vedotin in patients with relapsed or refractory diffuse large B-cell lymphoma. Leuk Lymphoma. 2020 Dec;61(12):2905-2914. doi: 10.1080/10428194.2020.1795154. Epub 2020 Jul 24. PMID: 32705923.
20: Bourbon E, Salles G. Polatuzumab vedotin: an investigational anti-CD79b antibody drug conjugate for the treatment of diffuse large B-cell lymphoma. Expert Opin Investig Drugs. 2020 Oct;29(10):1079-1088. doi: 10.1080/13543784.2020.1800638. Epub 2020 Aug 12. PMID: 32700972.
Chemical Structure
