WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130073
CAS#: 1989620-03-2
Description: PRT-543 is a selective oral PRMT5 inhibitor with a phase 1 clinical trial currently ongoing, testing its effectiveness as a treatment for solid tumors and hematologic malignancies. PRT-543 functions by selectively binding to the PRMT5 substrate recognition site, inhibiting methyltransferase, ultimately increasing the expression of anti-proliferative genes or decreasing expression of proliferative genes, which in turn can be used to prevent proliferation of cancer cells.
Hodoodo Cat#: H130073
Name: PRT-543
CAS#: 1989620-03-2
Chemical Formula: C17H17ClN4O4
Exact Mass: 376.09
Molecular Weight: 376.800
Elemental Analysis: C, 54.19; H, 4.55; Cl, 9.41; N, 14.87; O, 16.98
Synonym: PRT-543; PRT543; PRT 543; C220; PRMT5 inhibitor; PRMT5 inhibitor C220
IUPAC/Chemical Name: (2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-(4-chlorophenyl)-hydroxymethyl]oxolane-3,4-diol
InChi Key: ITEKIFMGFZAFPM-QFRSUPTLSA-N
InChi Code: InChI=1S/C17H17ClN4O4/c18-9-3-1-8(2-4-9)11(23)14-12(24)13(25)17(26-14)22-6-5-10-15(19)20-7-21-16(10)22/h1-7,11-14,17,23-25H,(H2,19,20,21)/t11-,12+,13-,14-,17-/m1/s1
SMILES Code: O[C@H]1[C@H](N2C=CC3=C(N)N=CN=C32)O[C@H]([C@@H](C4=CC=C(Cl)C=C4)O)[C@H]1O
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 376.80 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1. https://aacrjournals.org/mct/article/20/12_Supplement/P039/676075/Abstract-P039-A-phase-1-dose-escalation-study-of
2. https://clinicaltrials.gov/ct2/show/NCT03886831
3. https://www.cancer.gov/publications/dictionaries/cancer-drug/def/protein-arginine-methyltransferase-5-inhibitor-prt543