| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CDK9 8 nM (Ki)
CDK9 (cyclin-dependent kinase 9) and FLT3-ITD (FMS-like tyrosine kinase 3 internal tandem duplication). CDK9 is a kinase that regulates transcriptional elongation by phosphorylating RNA polymerase II at Ser2 and Ser5. FLT3-ITD is an oncogenic mutation found in approximately 30% of AML patients, driving leukemic cell proliferation and survival. CDDD11-8 inhibits both targets with high affinity (Ki = 8 nM for CDK9, 13 nM for FLT3-ITD). |
|---|---|
| ln Vitro |
CDDD11-8 (0-3 μM, 24 hours) inhibits the expression of c-MYC, MCL-1 and XIAP in MV4-11 and MOLM-13 cells [1]. CDDD11-8 dose-dependently inhibits proliferation (IC50 range: 281-734 nM), induces cell cycle arrest, and increases apoptosis in cell lines [2].
CDDD11-8 (0-3 μM, 24 h) suppresses the expressions of c-MYC, MCL-1, and XIAP in MV4-11 and MOLM-13 cells. It dose-dependently inhibits proliferation with IC50 values ranging from 281-734 nM, induces cell cycle arrest, and increases apoptosis of leukemia cell lines. It is particularly effective against cells harboring FLT3-ITD mutations. |
| ln Vivo |
CDDD11-8 (0-125 mg/kg, orally, daily) can induce tumor regression [1].
CDDD11-8 (0-125 mg/kg, PO, daily) induces tumor regression. In an animal model using MV4-11 tumor-bearing mice, the compound was tested at dosages of either 75 or 125 mg/kg administered orally on a daily basis for either 5 or 28 days. Results confirmed potent inhibition of CDK9 in vivo, evidenced by reduced phosphorylation of RNAPII at Ser2 and Ser5, and decreased phosphorylation of FLT3 at Tyr591 and STAT5 at Tyr694. |
| Enzyme Assay |
In vitro kinase assays are performed using recombinant CDK9 or FLT3-ITD enzymes incubated with ATP substrate and varying concentrations of CDDD11-8. Phosphorylation of peptide substrates is measured by radiometric, fluorescence-based, or ELISA-based methods. IC50 or Ki values are determined from dose-response curves. CDDD11-8 shows Ki values of 8 nM for CDK9 and 13 nM for FLT3-ITD.
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| Cell Assay |
Leukemia cell lines (MV4-11, MOLM-13) are treated with CDDD11-8 at varying concentrations. Cell proliferation is measured using standard assays (MTT, CCK-8, CellTiter-Glo). Apoptosis is assessed by Annexin V/PI staining and caspase activation. Cell cycle analysis is performed by flow cytometry. Target engagement is confirmed by Western blotting for phosphorylated RNAPII (Ser2, Ser5), phosphorylated FLT3 (Tyr591), and phosphorylated STAT5 (Tyr694).
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| Animal Protocol |
Animal/Disease Models: MV4-11 tumor-bearing mice[1]
Doses: 75 or 125 mg/kg Route of Administration: PO, daily for 5 or 28 days Experimental Results: Induced tumor regression. Potently inhibited the phosphorylation of RNAPII at Ser2 and Ser5, confirming the inhibition of CDK9 in vivo. Reduced phosphorylation of FLT3 at Tyr591 and STAT5 at Tyr 694. MV4-11 tumor-bearing mice are administered CDDD11-8 via oral gavage at dosages of 75 or 125 mg/kg daily for 5 or 28 days. Tumor volume is measured regularly using calipers. Tumor regression is induced by treatment. At study endpoint, tumors are collected for Western blotting analysis to confirm inhibition of CDK9 and FLT3 signaling. |
| ADME/Pharmacokinetics |
CDDD11-8 is orally active with favorable pharmacokinetic properties. It is absorbed after oral administration and reaches therapeutic concentrations in plasma. The compound is administered orally at doses up to 125 mg/kg daily in mouse models. Detailed PK parameters (Cmax, Tmax, AUC, t1/2) are available in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for CDDD11-8 are limited to preclinical studies. As a CDK9 and FLT3 inhibitor, potential toxicities may include myelosuppression, gastrointestinal effects, and cardiotoxicity. In animal models, doses up to 125 mg/kg were tolerated. Standard toxicology studies are required for therapeutic development. As a research compound, detailed toxicology data are not publicly available.
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| References | |
| Additional Infomation |
CDDD11-8 is a research-grade CDK9 and FLT3-ITD inhibitor for cancer research. CAS: 2241659-94-7. Molecular formula: C24H26N6, molecular weight: 398.50. Ki values: 8 nM (CDK9) and 13 nM (FLT3-ITD). It reduces proliferation of leukemia cell lines and induces tumor regression in xenograft models. For research use only, not for human therapeutic use.
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| Molecular Formula |
C24H26N6
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|---|---|
| Molecular Weight |
398.503444194794
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| Exact Mass |
398.221
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| CAS # |
2241659-94-7
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| PubChem CID |
135301300
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| Appearance |
Off-white to light brown solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CN=C(N=C1C2=CN=C3N2C=C(C=C3)C4=CC=CC=C4)NC5CCC(CC5)N
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| InChi Key |
OVOYRPVIZNJKHS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26N6/c1-16-13-27-24(28-20-10-8-19(25)9-11-20)29-23(16)21-14-26-22-12-7-18(15-30(21)22)17-5-3-2-4-6-17/h2-7,12-15,19-20H,8-11,25H2,1H3,(H,27,28,29)
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| Chemical Name |
4-N-[5-methyl-4-(6-phenylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]cyclohexane-1,4-diamine
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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 :~100 mg/mL (~250.94 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. 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 | 2.5094 mL | 12.5471 mL | 25.0941 mL | |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 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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