WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407203
Description: FRAX1036 is a potent and selective PAK1 inhibitor. Administration of docetaxel with either FRAX1036, or PAK1 small interfering RNA oligonucleotides dramatically altered signaling to cytoskeletal-associated proteins, such as stathmin, and induced microtubule disorganization and cellular apoptosis. Live-cell imaging revealed that the duration of mitotic arrest mediated by docetaxel was significantly reduced in the presence of FRAX1036, and this was associated with increased kinetics of apoptosis.
MedKoo Cat#: 407203
Chemical Formula: C28H32ClN7O
Exact Mass: 517.23569
Molecular Weight: 518.062
Elemental Analysis: C, 64.92; H, 6.23; Cl, 6.84; N, 18.93; O, 3.09
Synonym: FRAX1036; FRAX-1036; FRAX 1036.
IUPAC/Chemical Name: 6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
InChi Key: RYCBSFIKWACFBY-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H32ClN7O/c1-4-36-26-21(16-32-28(34-26)31-10-7-19-8-11-35(3)12-9-19)13-23(27(36)37)22-6-5-20(14-24(22)29)25-17-30-15-18(2)33-25/h5-6,13-17,19H,4,7-12H2,1-3H3,(H,31,32,34)
SMILES Code: O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
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 518.062 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: Mortazavi F, Lu J, Phan R, Lewis M, Trinidad K, Aljilani A, Pezeshkpour G,
Tamanoi F. Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer
oncogenesis. BMC Cancer. 2015 May 9;15:381. doi: 10.1186/s12885-015-1360-4.
PubMed PMID: 25956913; PubMed Central PMCID: PMC4477307.
2: Ong CC, Gierke S, Pitt C, Sagolla M, Cheng CK, Zhou W, Jubb AM, Strickland L,
Schmidt M, Duron SG, Campbell DA, Zheng W, Dehdashti S, Shen M, Yang N, Behnke
ML, Huang W, McKew JC, Chernoff J, Forrest WF, Haverty PM, Chin SF, Rakha EA,
Green AR, Ellis IO, Caldas C, O'Brien T, Friedman LS, Koeppen H, Rudolph J,
Hoeflich KP. Small molecule inhibition of group I p21-activated kinases in breast
cancer induces apoptosis and potentiates the activity of microtubule stabilizing
agents. Breast Cancer Res. 2015 Apr 23;17:59. doi: 10.1186/s13058-015-0564-5.
PubMed PMID: 25902869; PubMed Central PMCID: PMC4445529.