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Cayman PF-3758309
List Price $115.00 Your Price $115.00
Cayman PF-3758309 - CAYM (Additional S&H Or Hazmat Fees May Apply)
NETA PART: CAYM-19186-10
MFG.PART: 19186-10
UNSPSC: 12352200
Manufacturer: Cayman
Product Description
p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain. PAKs are upregulated in several human cancers and are potential therapeutic targets for cancer intervention. PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively). PF-3758309 blocks the growth of multiple human tumor xenografts.
WARNING This product is not for human or veterinary use.
Technical Information
Formal Name
N-
CAS Number
898044-15-0
Synonyms
- PF-309
Molecular Formula
C25H30N8OS
Formula Weight
490.6
Purity
≥98%
Formulation
A crystalline solid
Solubility
- DMF: 10 mg/mL
- DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL
- DMSO: 10 mg/mL
- Ethanol: 5 mg/mL
λmax
266, 312 nm
SMILES
CN(C)C[C@@H](NC(N1CC(C(NC2=NC(C)=NC3=C2SC=C3)=NN4)=C4C1(C)C)=O)C5=CC=CC=C5
InChi Code
InChI=1S/C25H30N8OS/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)/t19-/m1/s1
InChi Key
AYCPARAPKDAOEN-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room Temperature in continental US; may vary elsewhere
Stability
≥ 4 years
| SKU | CAYM-19186-10 |
|---|---|
| Supplier Part Number | 19186-10 |
| UM | EA |
| UNSPSC | 12352200 |
| Manufacturer | Cayman |
| MSDS URL | Click here |
| Temperature | -20 |
| Refrigerated-Frozen | Y |
| CountryOfOrigin | United States |
| ProductLine | CAYM |
| Qty | 1 |
| MinOrderQty | 1 |
| Weight | 7.000000 |
| Lead Time | 5 |
| Hazardous | Y |
| CAS Number | 898044-15-0 |
| Energy Star | No |
| Green | No |
| Controlled | N |