Madrasin
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MedKoo CAT#: 326823

CAS#: 374913-63-0

Description: Madrasin is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly. Madrasin stalls spliceosome assembly at the A complex.

Chemical Structure

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Madrasin
CAS# 374913-63-0
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 326823
Name: Madrasin
CAS#: 374913-63-0
Chemical Formula: C16H17N5O2
Exact Mass: 311.14
Molecular Weight: 311.345
Elemental Analysis: C, 61.72; H, 5.50; N, 22.49; O, 10.28

Price and Availability

Size Price Availability Quantity
10mg USD 90 Ready to ship
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 850 Ready to ship
500mg USD 1450 Ready to ship
1g USD 2450 Ready to ship
2g USD 3750 Ready to ship
5g USD 6950 2 weeks
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Synonym: DDD00107587; Madrasin. RNA splicing inhibitor

IUPAC/Chemical Name: 2-((7-Methoxy-4-methylquinazolin-2-yl)amino)-5,6-dimethylpyrimidin-4(3H)-one

InChi Key: QQJIYKXTEMDJFM-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N5O2/c1-8-9(2)17-16(20-14(8)22)21-15-18-10(3)12-6-5-11(23-4)7-13(12)19-15/h5-7H,1-4H3,(H2,17,18,19,20,21,22)

SMILES Code: O=C1NC(NC2=NC(C)=C3C=CC(OC)=CC3=N2)=NC(C)=C1C

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: 2934.99.9001

More Info:

Biological target: Madrasin (DDD00107587) is a pre-mRNA splicing inhibitor that prevents formation of both splicing intermediates and products in vitro and interferes with one or more early steps in the pathway of spliceosome assembly.
In vitro activity: To further determine the outcome of splicing defects in POLR2A, HeLa cells were treated with splicing inhibitor madrasin. RT-PCR and western blot revealed that POLR2A expression was down-regulated at RNA and protein levels (Figure3A–D). The inhibitory effect of madrasin on splicing was verified by RT-PCR as the treatment led to substantial increase of unspliced transcripts (Figure3E3E and F). Consistently, IF staining also supported that madrasin treatment resulted in POLR2A down-regulation (Figure3G). In addition, nascent RNA was markedly decreased after madrasin treatment by EU incorporation assay (Figure3H).Similarly, the expression of POLR2A in 293T or MDA-MB-231 cells was decreased at both RNA and protein levels when treated with madrasin (Supplementary Figure S7). These data together supported that splicing defects in POLR2A induced by XAB2 depletion was the major mechanism for decreased expression of POLR2A at RNA level. Reference: Nucleic Acids Res. 2019 Sep 5; 47(15): 8239–8254. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6735682/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 1.5 4.82

Preparing Stock Solutions

The following data is based on the product molecular weight 311.35 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.

Recalculate based on batch purity %
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
Formulation protocol: 1. Hou S, Qu D, Li Y, Zhu B, Liang D, Wei X, Tang W, Zhang Q, Hao J, Guo W, Wang W, Zhao S, Wang Q, Azam S, Khan M, Zhao H, Zhang L, Lei H. XAB2 depletion induces intron retention in POLR2A to impair global transcription and promote cellular senescence. Nucleic Acids Res. 2019 Sep 5;47(15):8239-8254. doi: 10.1093/nar/gkz532. PMID: 31216022; PMCID: PMC6735682. 2. Pawellek A, McElroy S, Samatov T, Mitchell L, Woodland A, Ryder U, Gray D, Lührmann R, Lamond AI. Identification of small molecule inhibitors of pre-mRNA splicing. J Biol Chem. 2014 Dec 12;289(50):34683-98. doi: 10.1074/jbc.M114.590976. Epub 2014 Oct 3. Erratum in: J Biol Chem. 2015 Mar 6;290(10):6005. PMID: 25281741; PMCID: PMC4263873.
In vitro protocol: 1. Hou S, Qu D, Li Y, Zhu B, Liang D, Wei X, Tang W, Zhang Q, Hao J, Guo W, Wang W, Zhao S, Wang Q, Azam S, Khan M, Zhao H, Zhang L, Lei H. XAB2 depletion induces intron retention in POLR2A to impair global transcription and promote cellular senescence. Nucleic Acids Res. 2019 Sep 5;47(15):8239-8254. doi: 10.1093/nar/gkz532. PMID: 31216022; PMCID: PMC6735682. 2. Pawellek A, McElroy S, Samatov T, Mitchell L, Woodland A, Ryder U, Gray D, Lührmann R, Lamond AI. Identification of small molecule inhibitors of pre-mRNA splicing. J Biol Chem. 2014 Dec 12;289(50):34683-98. doi: 10.1074/jbc.M114.590976. Epub 2014 Oct 3. Erratum in: J Biol Chem. 2015 Mar 6;290(10):6005. PMID: 25281741; PMCID: PMC4263873.
In vivo protocol: TBD

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