| Field | Specification |
|---|---|
| Target | |
| Alternative names | CAY-10572 hydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C12H12ClN3O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PHA-767491 hydrochloride, also known as CAY-10572 hydrochloride, is a dual Cdc7/Cdk9 inhibitor, with IC50 values of 10 nM and 34 nM, respectively. It is supplied as a light yellow to yellow solid (C12H12ClN3O, MW 249.70) at 99.49% purity.
Physical & Chemical Properties
| CAS Number | 942425-68-5 |
|---|---|
| Molecular Formula | C12H12ClN3O |
| Molecular Weight | 249.70 g/mol |
| Purity | 99.49% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | O=C1C2=C(NC(C3=CC=NC=C3)=C2)CCN1.[H]Cl |
| Target | CDK9, CDK2, CDK1, CDK5, GSK3-β, Mk2, Plk1, Chk2 |
| Signaling Pathway | Cell Cycle/DNA Damage; Apoptosis |
| Solubility | In Vitro: H2O: 50 mg/mL (200.24 mM; Requires sonication) DMSO: 17.33 mg/mL (69.40 mM; Requires sonication and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[4]
|
CDK9 34 nM (IC50) |
CDK2 240 nM (IC50) |
CDK1 250 nM (IC50) |
CDK5 460 nM (IC50) |
GSK3-β 220 nM (IC50) |
Mk2 470 nM (IC50) |
Plk1 980 nM (IC50) |
Chk2 1100 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | 50 mg/mL (200.24 mM) | requires sonication |
| DMSO | 17.33 mg/mL (69.40 mM) | requires sonication and warming; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 1 mg/mL (4.00 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1 mg/mL (4.00 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (10.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 3
| Composition | PBS |
|---|---|
| Result | 50 mg/mL (200.24 mM); clear solution; requires sonication |
Data provided by the manufacturer.
In Vitro
In both cell lines, PHA-767491 inhibits proliferation, with IC50 values of 0.64 μM (HCC1954 cells) and 1.3 μM (Colo-205 cells). PHA-767491 is an effective DDK inhibitor in vitro, with an IC50 of 18.6 nM. At 2 μM, PHA-767491 completely abolishes Mcm2 phosphorylation within 24 hours in HCC1954 cells[1]. Combined with 5-FU, PHA-767491 shows much stronger cytotoxicity and induces significant apoptosis, shown by markedly increased caspase 3 activation and fragmentation of poly(ADP-Ribose) polymerase in HCC cells. PHA-767491 directly counteracts 5-FU-induced Chk1 phosphorylation and reduces expression of the anti-apoptotic protein myeloid leukemia cell 1[2]. PHA-767491 (0-10 μM) reduces glioblastoma cell viability in a time- and dose-dependent fashion, with an IC50 of approximately 2.5 μM in both U87-MG and U251-MG cells. PHA-767491 hydrochloride induces apoptosis in glioblastoma cells and suppresses their proliferation, migration, and invasion[3].
In Vivo
In tumor tissue sections from nude mouse HCC xenografts, PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
CDK9 inhibition blocks the initiation of PINK1-PRKN-mediated mitophagy by regulating the SIRT1-FOXO3-BNIP3 axis and enhances the therapeutic effects involving mitochondrial dysfunction in hepatocellular carcinoma. Autophagy 2022 Aug;18(8):1879-1897. PMID: 34890308
CDK9 recruits HUWE1 to degrade RARα and offers therapeutic opportunities for cutaneous T-cell lymphoma. Nat Commun 2024 Dec 5;15(1):10594. PMID: 39632829
Novel CDK9 inhibitor oroxylin A promotes wild-type P53 stability and prevents hepatocellular carcinoma progression by disrupting both MDM2 and SIRT1 signaling. Acta Pharmacol Sin 2022 Apr;43(4):1033-1045. PMID: 34188177
Pre-therapeutic efficacy of the CDK inhibitor dinaciclib in medulloblastoma cells. Sci Rep 2021 Mar 8;11(1):5374. PMID: 33686114
CDK9 inhibition triggers MT2A-dependent apoptosis in HCC cells. Genes Genomics 2026 Jun;48(6):817-829. PMID: 41954877
