E7107 | CAS#630100-90-2 | spliceosome inhibitor

MedKoo Cat#: 562252 | Name: E7107

Description:

WARNING: This product is for research use only, not for human or veterinary use.

E7107 is a first-in-class precursor messenger ribonucleic acid (pre-mRNA) spliceosome inhibitor.

Chemical Structure

E7107

CAS#630100-90-2

Theoretical Analysis

MedKoo Cat#: 562252

Name: E7107

CAS#: 630100-90-2

Chemical Formula: C40H66N2O9

Exact Mass: 718.4768

Molecular Weight: 718.97

Elemental Analysis: C, 66.82; H, 9.25; N, 3.90; O, 20.03

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

Bulk Inquiry

Related CAS #

No Data

Synonym

E7107; E-7107; E 7107;

IUPAC/Chemical Name

[(2S,3S,4E,6S,7R,10R)-7,10-Dihydroxy-2-[(2E,4E,6R)-6-hydroxy-7-[(2R,3R)-3-[(2R,3S)-3-hydroxypentan-2-yl]oxiran-2-yl]-6-methylhepta-2,4-dien-2-yl]-3,7-dimethyl-12-oxo-1-oxacyclododec-4-en-6-yl] 4-cycloheptylpiperazine-1-carboxylate

InChi Key

MNOMBFWMICHMKG-MGYWSNOQSA-N

InChi Code

InChI=1S/C40H66N2O9/c1-7-32(44)29(4)37-33(49-37)26-39(5,47)19-12-13-27(2)36-28(3)16-17-34(40(6,48)20-18-31(43)25-35(45)51-36)50-38(46)42-23-21-41(22-24-42)30-14-10-8-9-11-15-30/h12-13,16-17,19,28-34,36-37,43-44,47-48H,7-11,14-15,18,20-26H2,1-6H3/b17-16+,19-12+,27-13+/t28-,29+,31+,32-,33+,34-,36+,37+,39-,40+/m0/s1

SMILES Code

O=C(N1CCN(C2CCCCCC2)CC1)O[C@H]([C@](C)(O)CC[C@@H](O)C3)/C=C/[C@H](C)[C@@H](/C(C)=C/C=C/[C@](C)(O)C[C@H]4O[C@@H]4[C@@H]([C@@H](O)CC)C)OC3=O

Appearance

Solid powder

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

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 718.97 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: Finci LI, Zhang X, Huang X, Zhou Q, Tsai J, Teng T, Agrawal A, Chan B, Irwin S, Karr C, Cook A, Zhu P, Reynolds D, Smith PG, Fekkes P, Buonamici S, Larsen NA. The cryo-EM structure of the SF3b spliceosome complex bound to a splicing modulator reveals a pre-mRNA substrate competitive mechanism of action. Genes Dev. 2018 Feb 1;32(3-4):309-320. doi: 10.1101/gad.311043.117. PubMed PMID: 29491137. 2: Núñez A, Núñez C, Corsi O, Rada G. Are cannabinoids effective for HIV wasting syndrome? Medwave. 2017 Dec 22;17(9):e7107. doi: 10.5867/medwave.2017.09.7107. Spanish, English. PubMed PMID: 29272264. 3: Chan S, Sridhar P, Kirchner R, Lock YJ, Herbert Z, Buonamici S, Smith P, Lieberman J, Petrocca F. Basal-A Triple-Negative Breast Cancer Cells Selectively Rely on RNA Splicing for Survival. Mol Cancer Ther. 2017 Dec;16(12):2849-2861. doi: 10.1158/1535-7163.MCT-17-0461. Epub 2017 Sep 6. PubMed PMID: 28878028. 4: Lee EP, Hsia SH, Huang JL, Lin JJ, Chan OW, Lin CY, Lin KL, Chang YC, Chou IJ, Lo FS, Lee J, Hsin YC, Chan PC, Hu MH, Chiu CH, Wu HP. Epidemiology and clinical analysis of critical patients with child maltreatment admitted to the intensive care units. Medicine (Baltimore). 2017 Jun;96(23):e7107. doi: 10.1097/MD.0000000000007107. PubMed PMID: 28591056; PubMed Central PMCID: PMC5466234. 5: Brierley CK, Steensma DP. Targeting Splicing in the Treatment of Myelodysplastic Syndromes and Other Myeloid Neoplasms. Curr Hematol Malig Rep. 2016 Dec;11(6):408-415. doi: 10.1007/s11899-016-0344-z. Review. PubMed PMID: 27492253. 6: Lee SC, Dvinge H, Kim E, Cho H, Micol JB, Chung YR, Durham BH, Yoshimi A, Kim YJ, Thomas M, Lobry C, Chen CW, Pastore A, Taylor J, Wang X, Krivtsov A, Armstrong SA, Palacino J, Buonamici S, Smith PG, Bradley RK, Abdel-Wahab O. Modulation of splicing catalysis for therapeutic targeting of leukemia with mutations in genes encoding spliceosomal proteins. Nat Med. 2016 Jun;22(6):672-8. doi: 10.1038/nm.4097. Epub 2016 May 2. Erratum in: Nat Med. 2016 Jun 7;22(6):692. PubMed PMID: 27135740; PubMed Central PMCID: PMC4899191. 7: Hong DS, Kurzrock R, Naing A, Wheler JJ, Falchook GS, Schiffman JS, Faulkner N, Pilat MJ, O'Brien J, LoRusso P. A phase I, open-label, single-arm, dose-escalation study of E7107, a precursor messenger ribonucleic acid (pre-mRNA) splicesome inhibitor administered intravenously on days 1 and 8 every 21 days to patients with solid tumors. Invest New Drugs. 2014 Jun;32(3):436-44. doi: 10.1007/s10637-013-0046-5. Epub 2013 Nov 22. PubMed PMID: 24258465. 8: Dehm SM. Test-firing ammunition for spliceosome inhibition in cancer. Clin Cancer Res. 2013 Nov 15;19(22):6064-6. doi: 10.1158/1078-0432.CCR-13-2461. Epub 2013 Oct 4. PubMed PMID: 24097858; PubMed Central PMCID: PMC3839097. 9: Eskens FA, Ramos FJ, Burger H, O'Brien JP, Piera A, de Jonge MJ, Mizui Y, Wiemer EA, Carreras MJ, Baselga J, Tabernero J. Phase I pharmacokinetic and pharmacodynamic study of the first-in-class spliceosome inhibitor E7107 in patients with advanced solid tumors. Clin Cancer Res. 2013 Nov 15;19(22):6296-304. doi: 10.1158/1078-0432.CCR-13-0485. Epub 2013 Aug 27. PubMed PMID: 23983259. 10: Dramatic trial results are often too good to be true. BMJ. 2012 Oct 24;345:e7107. doi: 10.1136/bmj.e7107. PubMed PMID: 23097542. 11: Folco EG, Lei H, Hsu JL, Reed R. Small-scale nuclear extracts for functional assays of gene-expression machineries. J Vis Exp. 2012 Jun 27;(64). pii: 4140. doi: 10.3791/4140. PubMed PMID: 22782264; PubMed Central PMCID: PMC3471294. 12: Folco EG, Coil KE, Reed R. The anti-tumor drug E7107 reveals an essential role for SF3b in remodeling U2 snRNP to expose the branch point-binding region. Genes Dev. 2011 Mar 1;25(5):440-4. doi: 10.1101/gad.2009411. PubMed PMID: 21363962; PubMed Central PMCID: PMC3049285. 13: Fan L, Lagisetti C, Edwards CC, Webb TR, Potter PM. Sudemycins, novel small molecule analogues of FR901464, induce alternative gene splicing. ACS Chem Biol. 2011 Jun 17;6(6):582-9. doi: 10.1021/cb100356k. Epub 2011 Mar 7. PubMed PMID: 21344922; PubMed Central PMCID: PMC3113647. 14: Ganesalingam J, Stahl D, Wijesekera L, Galtrey C, Shaw CE, Leigh PN, Al-Chalabi A. Latent cluster analysis of ALS phenotypes identifies prognostically differing groups. PLoS One. 2009 Sep 22;4(9):e7107. doi: 10.1371/journal.pone.0007107. PubMed PMID: 19771164; PubMed Central PMCID: PMC2741575.