WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206199
Description: Mavelertinib, also known as PF-06747775, is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. EGFR T790M inhibitor PF-06747775 specifically binds to and inhibits EGFR T790M, a secondarily acquired resistance mutation, which prevents EGFR-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. Compared to some other EGFR inhibitors, PF-06747775 may have therapeutic benefits in tumors with T790M-mediated drug resistance.
MedKoo Cat#: 206199
Chemical Formula: C18H22FN9O2
Exact Mass: 415.188
Molecular Weight: 415.4334
Elemental Analysis: C, 52.04; H, 5.34; F, 4.57; N, 30.34; O, 7.70
Synonym: PF06747775; PF06747775; PF 06747775; PF6747775; PF 6747775; PF6747775; mavelertinib;
IUPAC/Chemical Name: N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidin-3-yl)acrylamide
InChi Key: JYIUNVOCEFIUIU-GHMZBOCLSA-N
InChi Code: InChI=1S/C18H22FN9O2/c1-5-13(29)21-11-8-28(6-10(11)19)18-23-15(14-16(24-18)26(2)9-20-14)22-12-7-27(3)25-17(12)30-4/h5,7,9-11H,1,6,8H2,2-4H3,(H,21,29)(H,22,23,24)/t10-,11-/m1/s1
SMILES Code: C=CC(N[C@@H]1CN(C2=NC(NC3=CN(C)N=C3OC)=C4N=CN(C)C4=N2)C[C@H]1F)=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, not in water
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
The following data is based on the product molecular weight 415.4334 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: Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S,
Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM,
Edwards MP, Ferre RA, Gajiwala KS, Hemkens MD, Kania RS, Kath JC, Matthews J,
Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran
K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin
S, Zhang C, Lafontaine JA. Discovery of
purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) Through Structure-Based Drug
Design; A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants
With Selectivity Over Wild-Type EGFR. J Med Chem. 2017 Mar 13. doi:
10.1021/acs.jmedchem.6b01894. [Epub ahead of print] PubMed PMID: 28287730.
2: Wang S, Cang S, Liu D. Third-generation inhibitors targeting EGFR T790M
mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr
12;9:34. doi: 10.1186/s13045-016-0268-z. Review. PubMed PMID: 27071706; PubMed
Central PMCID: PMC4830020.