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MedKoo Cat#: 206975 | Name: PF-06855800
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Description:

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

PF-06855800 is a SAM competitive PRMT5 inhibitor with antiproliferative activity in both in vitro and in vivo models.

Chemical Structure

PF-06855800
PF-06855800
CAS#1989620-04-3

Theoretical Analysis

MedKoo Cat#: 206975

Name: PF-06855800

CAS#: 1989620-04-3

Chemical Formula: C17H16ClFN4O4

Exact Mass: 394.0844

Molecular Weight: 394.79

Elemental Analysis: C, 51.72; H, 4.09; Cl, 8.98; F, 4.81; N, 14.19; O, 16.21

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
10mg USD 750.00 2 Weeks
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Related CAS #
No Data
Synonym
PF-06855800; PF06855800; PF06855800;
IUPAC/Chemical Name
(2R,3R,4S,5R)-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-((R)-(4-chloro-3-fluorophenyl)(hydroxy)methyl)tetrahydrofuran-3,4-diol
InChi Key
GTCYWLXMJRCJNE-QFRSUPTLSA-N
InChi Code
InChI=1S/C17H16ClFN4O4/c18-9-2-1-7(5-10(9)19)11(24)14-12(25)13(26)17(27-14)23-4-3-8-15(20)21-6-22-16(8)23/h1-6,11-14,17,24-26H,(H2,20,21,22)/t11-,12+,13-,14-,17-/m1/s1
SMILES Code
NC1=C2C(N([C@H]3[C@@H]([C@@H]([C@@H]([C@@H](C4=CC=C(Cl)C(F)=C4)O)O3)O)O)C=C2)=NC=N1
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
Protein arginine methyltransferase 5 (PRMT5) is the primary type II arginine methyltransferase responsible for symmetric dimethylation of protein arginine residues. PRMT5 utilizes S-adenosylmethionine (SAM) to methylate a number of cytoplasmic and nuclear substrates that are involved in tumorigenesis.

Preparing Stock Solutions

The following data is based on the product molecular weight 394.79 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
Jensen-Pergakes, K., Tatlock, J., Maegley, K. A., McAlpine, I. J., McTigue, M., Xie, T., ... & Paul, T. A. (2022). SAM-competitive PRMT5 inhibitor PF-06939999 demonstrates antitumor activity in splicing dysregulated NSCLC with decreased liability of drug resistance. Molecular cancer therapeutics, 21(1), 3-15. Font, H., & Fernandez Forner, D. (2018). American Chemical Society-255th National Meeting and Exhibition. New Orleans, Louisiana, USA-March 18-22, 2018. Drugs of the Future, 43(5). Lin, H., & Luengo, J. I. (2019). Nucleoside protein arginine methyltransferase 5 (PRMT5) inhibitors. Bioorganic & Medicinal Chemistry Letters, 29(11), 1264-1269. Mcalpine, I. J., Tatlock, J., Billitti, J., Braganza, J., Brooun, A., Ya-Li, D., ... & Wythes, M. (2018). Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity. Cancer Research, 78(13_Supplement), 4857-4857. Guo, C., Wu, L., Zheng, X., Zhao, L., Hou, X., Wang, Z., & Han, C. (2023). Research Progress on Small-molecule Inhibitors of Protein Arginine Methyltransferase 5 (PRMT5) for Treating Cancer. Current Topics in Medicinal Chemistry, 23(21), 2048-2074.

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