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FRAX1036 (FRAX-1036; FRAX 1036) is a selective p21-activated kinase 1 (PAK1) inhibitor with potential anticancer activity. With Ki values of 23.3 nM and 72.4 nM, respectively, it inhibits PAK1 and PAK2.
| Targets |
PAK1 (Ki = 23.3 nM); PAK2 (Ki = 72.4 nM); PAK4 (Ki = 2.4 μM)
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| ln Vitro |
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| ln Vivo |
Frax1036 treatment slows the growth of KT21 tumors and is unlikely to cause significant blood brain barrier permeability in mice.
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| Enzyme Assay |
The phosphorylation of a FRET peptide substrate (Ser/Thr19) labeled with coumarin and fluorescein is measured using the Z'-LYTETM assay to determine the activity/inhibition of human recombinant PAK1 (kinase domain), PAK2 (full length), or PAK4 (kinase domain). The samples used in the 10 μL assay mixtures include 20 pM PAK1; 50 pM PAK2; 90 pM PAK4), 0.01% Brij-35, 10 mM MgCl2, 1 mM EGTA, and 50 mM HEPES (pH 7.5). In black polypropylene 384-well plates, incubations are conducted at 22°C. The assay is started by adding 2.5 μL of assay buffer containing 4× ATP (160 μM PAK1; 480 μM PAK2; 16 μM PAK4). The enzyme, FRET peptide substrate, and serially diluted test compounds (FRAX1036, etc.) are preincubated together in assay buffer (7.5 μL) for 10 minutes prior to the assay. After the assay mixtures are incubated for 60 minutes, 5 μL of Z'-LYTETM development reagent is added to quench them, and an hour later, the emissions of fluorescein (520 nm) and coumarin (445 nm) are measured following excitation at 400 nm. A measurement is made of the emission ratio (445 nm/520 nm) to determine the extent of substrate phosphorylation[1].
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| Cell Assay |
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| Animal Protocol |
Pak2-deficient mice
30 mg/kg by oral gavage |
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| References |
| Molecular Formula |
C28H32CLN7O
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| Molecular Weight |
518.062
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| Exact Mass |
517.23569
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| Elemental Analysis |
C, 64.92; H, 6.23; Cl, 6.84; N, 18.93; O, 3.09
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| CAS # |
1432908-05-8
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| Related CAS # |
1432908-05-8
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| Appearance |
Solid powder
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| SMILES |
CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)C4=NC(=CN=C4)C)Cl)NCCC5CCN(CC5)C
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| InChi Key |
RYCBSFIKWACFBY-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-one
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| Synonyms |
FRAX 1036; FRAX-1036; FRAX1036
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5.3 mg/mL (~10.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (19.30 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9303 mL | 9.6514 mL | 19.3028 mL | |
| 5 mM | 0.3861 mL | 1.9303 mL | 3.8606 mL | |
| 10 mM | 0.1930 mL | 0.9651 mL | 1.9303 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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