| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
PF-06651481-00 targets Src and Abl kinases as a dual inhibitor. As an isomer of Bosutinib, it would be expected to inhibit Bcr-Abl kinase activity, which is the molecular driver of Philadelphia chromosome-positive CML. The compound may also have binding affinity for Wee1 and Wee2 kinases, with reported Kd values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively.
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| ln Vitro |
The growth inhibitory potential of bosutinib isomers (0-10 μM) against HEK293T, MM1.S, and MDA-MB-231 cells is high; their respective IC50 values are 1.6 ± 0.19, 3.9 ± 0.50, and 1.8 ± 0.061 μM. [1].
In vitro activity data for PF-06651481-00 are not extensively detailed in the available literature. As an isomer of Bosutinib, it would be expected to demonstrate potent inhibition of Src and Abl kinases. The compound shows high binding affinity for Wee1 and Wee2 kinases with Kd values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively. |
| ln Vivo |
In vivo activity data for PF-06651481-00 are not extensively detailed in the available literature. As an isomer of Bosutinib, it would be expected to have antitumor activity in vivo, similar to the approved drug Bosutinib. Specific in vivo efficacy data for this isomer are not reported.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PF-06651481-00 involve kinase inhibition assays. Binding affinity for Src, Abl, Wee1, and Wee2 kinases is determined using radioligand binding or biochemical kinase activity assays. Kd values of 43.7 ± 10.0 nM (Wee1) and 4.7 ± 2.3 nM (Wee2) have been reported.
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| Cell Assay |
In vitro cell-based assays for PF-06651481-00 use cancer cell lines to assess antiproliferative activity. As an isomer of Bosutinib, the compound would be evaluated in Bcr-Abl-positive leukemia cell lines to measure inhibition of cell proliferation and kinase signaling. Specific assay protocols for this isomer are not detailed in the available literature.
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| Animal Protocol |
In vivo animal studies for PF-06651481-00 are not detailed in the available literature. As a Bosutinib isomer, typical in vivo evaluation would involve xenograft mouse models bearing Bcr-Abl-positive tumors to assess antitumor efficacy and pharmacokinetic properties.
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| ADME/Pharmacokinetics |
PF-06651481-00 has a molecular formula of C26H29Cl2N5O3 and a molecular weight of approximately 530.45 g/mol. It is soluble in DMSO at 10 mg/mL (warmed). Storage: powder at -20°C for 3 years or 4°C for 2 years. The compound is an isomer of the orally available dual Src/Abl kinase inhibitor Bosutinib.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PF-06651481-00 are not detailed in the available literature. The compound is classified as a combustible solid (Storage Class 11) with WGK 3. It is intended for laboratory research use only and is not for human use.
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| References | |
| Additional Infomation |
PF-06651481-00 (CAS 1391063-17-4) is an isomer of the orally available dual Src/Abl kinase inhibitor Bosutinib, an approved drug for Philadelphia chromosome-positive CML. It shows binding affinity for Wee1 and Wee2 kinases with Kd values of 43.7 nM and 4.7 nM, respectively. The compound is used in kinase research. No clinical trial data are available.
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| Molecular Formula |
C26H29CL2N5O3
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|---|---|
| Molecular Weight |
530.45
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| Exact Mass |
529.165
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| CAS # |
1391063-17-4
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| Related CAS # |
Bosutinib;380843-75-4
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| PubChem CID |
60202320
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.139
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
722
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YCLIWTLPTXAGPQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-24-14-22-19(13-23(24)34-2)25(17(15-29)16-30-22)31-18-11-20(27)26(35-3)21(28)12-18/h11-14,16H,4-10H2,1-3H3,(H,30,31)
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| Chemical Name |
4-(3,5-dichloro-4-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
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| Synonyms |
PF0665148100 Bosutinib Isomer I PF 06651481 00 PF-06651481-00
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8852 mL | 9.4260 mL | 18.8519 mL | |
| 5 mM | 0.3770 mL | 1.8852 mL | 3.7704 mL | |
| 10 mM | 0.1885 mL | 0.9426 mL | 1.8852 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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