MedKoo Cat#: 465729 | Name: PF-06939999

Description:

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

PF-06939999 is a potent and selective SAM Competitive PRMT5 Inhibitor. PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance. PRMT5 inhibition by PF-06939999 treatment reduced proliferation of NSCLC cancer cells, with dose-dependent decreases in symmetric dimethyl arginine (SDMA) levels and changes in alternative splicing of numerous pre-mRNAs. Drug sensitivity to PF-06939999 in NSCLC cells associates with cancer pathways including MYC, cell cycle and spliceosome, and with mutations in splicing factors such as RBM10.

Chemical Structure

PF-06939999
PF-06939999
CAS#2159123-14-3

Theoretical Analysis

MedKoo Cat#: 465729

Name: PF-06939999

CAS#: 2159123-14-3

Chemical Formula: C22H23F3N4O3

Exact Mass: 448.1722

Molecular Weight: 448.45

Elemental Analysis: C, 58.92; H, 5.17; F, 12.71; N, 12.49; O, 10.70

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.
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Related CAS #
No Data
Synonym
PF-06939999; PF06939999; PF 06939999; PRMT5-IN-3;
IUPAC/Chemical Name
(1S,2S,5R)-3-((6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl)oxy)-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol
InChi Key
HBGHQRGHFNTSDP-DGJRPJRTSA-N
InChi Code
InChI=1S/C22H23F3N4O3/c1-10-11-3-5-29(22(11)28-9-27-10)15-7-17(20(31)19(15)30)32-16-6-13(21(24)25)18(23)12-2-4-26-8-14(12)16/h3,5-6,9,15,17,19-21,26,30-31H,2,4,7-8H2,1H3/t15-,17?,19+,20-/m1/s1
SMILES Code
O[C@@H]1C(OC2=CC(C(F)F)=C(F)C3=C2CNCC3)C[C@@H](N4C(N=CN=C5C)=C5C=C4)[C@@H]1O
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
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

Preparing Stock Solutions

The following data is based on the product molecular weight 448.45 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
1: Jensen-Pergakes K, Tatlock J, Maegley KA, McAlpine IJ, McTigue M, Xie T, Dillon CP, Wang Y, Yamazaki S, Spiegel N, Shi M, Nemeth A, Miller N, Hendrickson E, Lam H, Sherrill J, Chung CY, McMillan EA, Bryant SK, Palde P, Braganza J, Brooun A, Deng YL, Goshtasbi V, Kephart SE, Kumpf RA, Liu W, Patman RL, Rui E, Scales S, Tran-Dube M, Wang F, Wythes M, Paul TA. SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance. Mol Cancer Ther. 2022 Jan;21(1):3-15. doi: 10.1158/1535-7163.MCT-21-0620. Epub 2021 Nov 4. PMID: 34737197.