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PD153035 hydrochloride

Cat. No. M3689
PD153035 hydrochloride Structure
Synonym:

ZM 252868, AG 1517

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 50  USD50 In stock
10mg USD 65  USD65 In stock
50mg USD 240  USD240 In stock
100mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

PD153035 hydrochloride (ZM 252868, AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. PD153035 HCl shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively. PD153035 induces a dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC) cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of 12.9 μM, 9.8 μM and 18.6μM, respectively. PD 153035 inhibits other purified tyrosine kinases only at micromolar or higher concentrations.

Protocol (for reference only)
Cell Experiment
Cell lines A431, Difi, DU145, MDA-MB-468 and ME180
Preparation method Seeding cells in sixwell plates. The next day, changing cells to medium containing 0.5% FBS for 18 hours, and then adding PD153035 at various concentrations to the cultures. After 72 hours of treatment, washing cells once with PBS, harvesting with 0.1% human trypsin-l mM EDTA in PBS, and counting with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.
Concentrations 0-3 μM
Incubation time 72 hours
Animal Experiment
Animal models A431 cells are injected into the outbred nude mice
Formulation PD153035 is dissolved in water.
Dosages ≤80 mg/kg
Administration Administered via i.p.
Chemical Information
Molecular Weight 396.67
Formula C16H14BrN3O2.HCl
CAS Number 183322-45-4
Solubility (25°C) DMSO 4 mg/mL (Need ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hsu CH, et al. Oncology. Inhibitors of epidermoid growth factor receptor suppress cell growth and enhance chemosensitivity of nasopharyngeal cancer cells in vitro.

[2] Bridges AJ, et al. J Med Chem. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.

[3] Fry DW, et al. Science. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase.

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Keywords: PD153035 hydrochloride, ZM 252868, AG 1517 supplier, EGFR/HER2, inhibitors, activators


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