PD153035 HCl
Modify Date: 2024-01-02 18:45:31
PD153035 HCl structure
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Common Name | PD153035 HCl | ||
|---|---|---|---|---|
| CAS Number | 183322-45-4 | Molecular Weight | 396.666 | |
| Density | N/A | Boiling Point | 472.1ºC at 760 mmHg | |
| Molecular Formula | C16H15BrClN3O2 | Melting Point | 265°C(lit.) | |
| MSDS | Chinese USA | Flash Point | 239.3ºC | |
| Symbol |
GHS05, GHS06 |
Signal Word | Danger | |
Use of PD153035 HClPD153035 (ZM 252868;AG 1517;Tyrphostin AG 1517;SU 5271) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively. |
| Name | N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine,hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | PD153035 (ZM 252868;AG 1517;Tyrphostin AG 1517;SU 5271) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively. |
|---|---|
| Related Catalog | |
| Target |
EGFR:6 pM (Ki) EGFR:25 pM (IC50) |
| In Vitro | PD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM[1]. PD 153035 has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD 153035 rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation[2]. PD153035 causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC50 is less than 1 pM in most cases[3]. |
| In Vivo | PD153035 levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD 153035 falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors[4]. |
| Cell Assay | Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed[3]. |
| Animal Admin | Mice: Mice are injected with PD153035 (80 mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD 153035 of the EGF-stimulation[3]. |
| References |
| Boiling Point | 472.1ºC at 760 mmHg |
|---|---|
| Melting Point | 265°C(lit.) |
| Molecular Formula | C16H15BrClN3O2 |
| Molecular Weight | 396.666 |
| Flash Point | 239.3ºC |
| Exact Mass | 395.003601 |
| PSA | 56.27000 |
| LogP | 5.02810 |
| Appearance of Characters | white to beige |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: soluble2mg/mL, clear (warmed) |
| Symbol |
GHS05, GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H315-H318-H335 |
| Precautionary Statements | P261-P280-P301 + P310-P305 + P351 + P338 |
| Hazard Codes | T |
| Risk Phrases | 25-37/38-41 |
| Safety Phrases | 26-39-45 |
| RIDADR | UN 2811 6.1 / PGIII |
| HS Code | 2933990090 |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Mesenchymal transition and dissemination of cancer cells is driven by myeloid-derived suppressor cells infiltrating the primary tumor.
PLoS Biol. 9 , e1001162, (2011) In order to metastasize, cancer cells need to acquire a motile phenotype. Previously, development of this phenotype was thought to rely on the acquisition of selected, random mutations and thus would ... |
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Reduced annexin A6 expression promotes the degradation of activated epidermal growth factor receptor and sensitizes invasive breast cancer cells to EGFR-targeted tyrosine kinase inhibitors.
Mol. Cancer 12 , 167, (2014) The expression of annexin A6 (AnxA6) in AnxA6-deficient non-invasive tumor cells has been shown to terminate epidermal growth factor receptor (EGFR) activation and downstream signaling. However, as a ... |
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Claudin-2 expression increases tumorigenicity of colon cancer cells: role of epidermal growth factor receptor activation.
Oncogene 30 , 3234-47, (2011) Claudin-2 is a unique member of the claudin family of transmembrane proteins, as its expression is restricted to the leaky epithelium in vivo and correlates with epithelial leakiness in vitro. However... |
| Tyrphostin AG 1517 |
| N-(3-Bromophenyl)-6,7-dimethoxy-4-quinazolinamine hydrochloride (1:1) |
| N-(3-Bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride |
| PD-153035 HYDROCHLORIDE |
| 4-[(3-BROMOPHENYL)AMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE |
| 4-Quinazolinamine, N-(3-bromophenyl)-6,7-dimethoxy-, hydrochloride (1:1) |
| N-(3-Bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride (1:1) |
| PD153035 HCl |
| PD153035 HCL |
| SU-5271 |
| AG1517 |
| PD153035 Hydrochloride |
- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: PD153035 HCl
- Price: ￥738.0/10mg ￥1678.0/50mg ￥5478.0/250mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: PD153035 HCl (SU-5271, AG1517)
- Price: $350.0/100mg $650.0/250mg $1300.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: N-(3-BROMOPHENYL)-6,7-DIMETHOXYQUINAZOLIN-4-AMINE HYDROCHLORIDE
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Ms Wang
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Price: $66/10mM*1mLinDMSO
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