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MedKoo Cat#: 125449 | Name: PF-03758309 HCl

Description:

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

PF-3758309, also known as PF-03758309, is a PAK4 inhibitor, is also an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PAK4 inhibitor PF-03758309 binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

Chemical Structure

PF-03758309 HCl
PF-03758309 HCl
CAS#1279034-84-2 (HCl)

Theoretical Analysis

MedKoo Cat#: 125449

Name: PF-03758309 HCl

CAS#: 1279034-84-2 (HCl)

Chemical Formula: C25H31ClN8OS

Exact Mass: 526.2000

Molecular Weight: 527.09

Elemental Analysis: C, 56.97; H, 5.93; Cl, 6.73; N, 21.26; O, 3.04; S, 6.08

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 #
898044-15-0 (free base) 1279034-84-2 (HCl)
Synonym
PF-03758309 hydrochloride; 1279034-84-2; PF-03758309 hydrochloride salt; UNII-BS52H27235; BS52H27235
IUPAC/Chemical Name
(S)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-((2-methylthieno[3,2-d]pyrimidin-4-yl)amino)-2,6-dihydropyrrolo[3,4-c]pyrazole-5(4H)-carboxamide hydrochloride
InChi Key
DZSGSCZKFHGJNK-FSRHSHDFSA-N
InChi Code
InChI=1S/C25H30N8OS.ClH/c1-15-26-18-11-12-35-20(18)23(27-15)29-22-17-13-33(25(2,3)21(17)30-31-22)24(34)28-19(14-32(4)5)16-9-7-6-8-10-16;/h6-12,19H,13-14H2,1-5H3,(H,28,34)(H2,26,27,29,30,31);1H/t19-;/m1./s1
SMILES Code
Cl.CN(C)C[C@@H](NC(=O)N1CC2=C(NC3=C4SC=CC4=NC(C)=N3)NN=C2C1(C)C)C5=CC=CC=C5
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

Preparing Stock Solutions

The following data is based on the product molecular weight 527.09 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: Briz V, Baudry M. Estrogen Regulates Protein Synthesis and Actin Polymerization in Hippocampal Neurons through Different Molecular Mechanisms. Front Endocrinol (Lausanne). 2014 Feb 25;5:22. doi: 10.3389/fendo.2014.00022. eCollection 2014. PubMed PMID: 24611062; PubMed Central PMCID: PMC3933789. 2: Fu X, Feng J, Zeng D, Ding Y, Yu C, Yang B. PAK4 confers cisplatin resistance in gastric cancer cells via PI3K/Akt- and MEK/Erk-dependent pathways. Biosci Rep. 2014 Jan 29. [Epub ahead of print] PubMed PMID: 24471762; PubMed Central PMCID: PMC3941610. 3: Ryu BJ, Lee H, Kim SH, Heo JN, Choi SW, Yeon JT, Lee J, Lee J, Cho JY, Kim SH, Lee SY. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings. Mol Cell Biochem. 2014 Apr;389(1-2):69-77. doi: 10.1007/s11010-013-1928-8. Epub 2013 Dec 24. PubMed PMID: 24366569. 4: Gao J, Ha BH, Lou HJ, Morse EM, Zhang R, Calderwood DA, Turk BE, Boggon TJ. Substrate and inhibitor specificity of the type II p21-activated kinase, PAK6. PLoS One. 2013 Oct 28;8(10):e77818. doi: 10.1371/journal.pone.0077818. eCollection 2013. PubMed PMID: 24204982; PubMed Central PMCID: PMC3810134. 5: Itakura A, Aslan JE, Kusanto BT, Phillips KG, Porter JE, Newton PK, Nan X, Insall RH, Chernoff J, McCarty OJ. p21-Activated kinase (PAK) regulates cytoskeletal reorganization and directional migration in human neutrophils. PLoS One. 2013 Sep 3;8(9):e73063. doi: 10.1371/journal.pone.0073063. eCollection 2013. PubMed PMID: 24019894; PubMed Central PMCID: PMC3760889. 6: Arias-Romero LE, Villamar-Cruz O, Huang M, Hoeflich KP, Chernoff J. Pak1 kinase links ErbB2 to β-catenin in transformation of breast epithelial cells. Cancer Res. 2013 Jun 15;73(12):3671-82. doi: 10.1158/0008-5472.CAN-12-4453. Epub 2013 Apr 10. PubMed PMID: 23576562; PubMed Central PMCID: PMC3687032. 7: Pitts TM, Kulikowski GN, Tan AC, Murray BW, Arcaroli JJ, Tentler JJ, Spreafico A, Selby HM, Kachaeva MI, McPhillips KL, Britt BC, Bradshaw-Pierce EL, Messersmith WA, Varella-Garcia M, Eckhardt SG. Association of the epithelial-to-mesenchymal transition phenotype with responsiveness to the p21-activated kinase inhibitor, PF-3758309, in colon cancer models. Front Pharmacol. 2013 Mar 28;4:35. doi: 10.3389/fphar.2013.00035. eCollection 2013. PubMed PMID: 23543898; PubMed Central PMCID: PMC3610060. 8: Ong CC, Jubb AM, Jakubiak D, Zhou W, Rudolph J, Haverty PM, Kowanetz M, Yan Y, Tremayne J, Lisle R, Harris AL, Friedman LS, Belvin M, Middleton MR, Blackwood EM, Koeppen H, Hoeflich KP. P21-activated kinase 1 (PAK1) as a therapeutic target in BRAF wild-type melanoma. J Natl Cancer Inst. 2013 May 1;105(9):606-7. doi: 10.1093/jnci/djt054. Epub 2013 Mar 27. PubMed PMID: 23535073. 9: Bradshaw-Pierce EL, Pitts TM, Tan AC, McPhillips K, West M, Gustafson DL, Halsey C, Nguyen L, Lee NV, Kan JL, Murray BW, Eckhardt SG. Tumor P-Glycoprotein Correlates with Efficacy of PF-3758309 in in vitro and in vivo Models of Colorectal Cancer. Front Pharmacol. 2013 Mar 22;4:22. doi: 10.3389/fphar.2013.00022. eCollection 2013. PubMed PMID: 23524533; PubMed Central PMCID: PMC3605511. 10: Chow HY, Jubb AM, Koch JN, Jaffer ZM, Stepanova D, Campbell DA, Duron SG, O'Farrell M, Cai KQ, Klein-Szanto AJ, Gutkind JS, Hoeflich KP, Chernoff J. p21-Activated kinase 1 is required for efficient tumor formation and progression in a Ras-mediated skin cancer model. Cancer Res. 2012 Nov 15;72(22):5966-75. doi: 10.1158/0008-5472.CAN-12-2246. Epub 2012 Sep 14. PubMed PMID: 22983922; PubMed Central PMCID: PMC3500416. 11: Maruta H. Effective neurofibromatosis therapeutics blocking the oncogenic kinase PAK1. Drug Discov Ther. 2011 Dec;5(6):266-78. PubMed PMID: 22466437. 12: Zhao ZS, Manser E. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70. doi: 10.3410/B2-70. PubMed PMID: 21173843; PubMed Central PMCID: PMC2989626. 13: Murray BW, Guo C, Piraino J, Westwick JK, Zhang C, Lamerdin J, Dagostino E, Knighton D, Loi CM, Zager M, Kraynov E, Popoff I, Christensen JG, Martinez R, Kephart SE, Marakovits J, Karlicek S, Bergqvist S, Smeal T. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51. doi: 10.1073/pnas.0911863107. Epub 2010 May 3. PubMed PMID: 20439741; PubMed Central PMCID: PMC2889050.

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