L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
![L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2) Structure](CAS/GIF/685898-44-6.gif)
- CAS No.
- 685898-44-6
- Chemical Name:
- L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2)
- Synonyms
- CS-1467;PX-478 HCl;PX478 2HCl;ALKN004012;PX478 2HCI;PX 478 DISCONTINUED;PX-478, 10 mM in DMSO;PX-478 dihydrochloride;4-[Bis(2-chloroethyl)oxidoamino]-L-phenylalanine dihydrochloride;4-[bis(2-chloroethyl)oxidoamino]-L-phenylalanine,hydrochloride (1:2)
- CBNumber:
- CB02628046
- Molecular Formula:
- C13H19Cl3N2O3
- Molecular Weight:
- 357.66
- MDL Number:
- MFCD11840749
- MOL File:
- 685898-44-6.mol
- MSDS File:
- SDS
| storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
|---|---|
| solubility | ≥19.7 mg/mL in DMSO; ≥50 mg/mL in H2O; ≥8.42 mg/mL in EtOH |
| form | Powder |
| color | Off-white to yellow |
| CAS DataBase Reference | 685898-44-6 |
| FDA UNII | T23U22X160 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 | |||||||||
| NFPA 704 |
|
L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2) price More Price(25)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 10005189 | PX-478 ≥95% | 685898-44-6 | 5mg | $66 | 2024-03-01 | Buy |
| Cayman Chemical | 10005189 | PX-478 ≥95% | 685898-44-6 | 50mg | $387 | 2024-03-01 | Buy |
| Cayman Chemical | 10005189 | PX-478 ≥95% | 685898-44-6 | 1mg | $30 | 2021-12-16 | Buy |
| Cayman Chemical | 10005189 | PX-478 ≥95% | 685898-44-6 | 10mg | $117 | 2024-03-01 | Buy |
| Cayman Chemical | 10005189 | PX-478 ≥95% | 685898-44-6 | 25mg | $259 | 2024-03-01 | Buy |
L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2) Chemical Properties,Uses,Production
Uses
PX 478 is a HIF-1α inhibitor that may be used in cancer therapy for treatment of solid tumors. PX478 has also been shown to suppress high-fat-diet (HFD)-induced HIFα activation in adipose tissue in mice and therefore may be used to ameliorate adipose tissue dysfunction.
Biological Activity
px-478 2hcl, also called px-478, is an experimental hif-1α inhibitor. it inhibited hif-1α protein at multiple levels in cancer cell lines under normoxia and hypoxia with an ic50 value of ~20-30 μm [1].hypoxia-inducible transcription factor hif-1α activates target genes involved in glycolysis, erythropoiesis and angiogenesis. hif-1α also regulates the expression of genes coding for apoptotic pathway, growth factors/receptors, cell cycle regulators, metastasis and invasiveness [1].under normoxic condition, the ic50 for px-478 to inhibit hif-1α in pc3 cells was 20-25 μmol/l, whereas the ic50 for px-478 to inhibit hif-1α in the du 145 cells was ~40-50 μmol/l. in both du 145 and pc3 cells, 1-hr hypoxia significantly upregulated hif-1α protein. but the pretreatment with px-478 for 20 hr under normoxia before 1-hr hypoxia attenuated the accumulation of hif-1α induced by the 1-hr hypoxia. in pc3 cells, pretreatment with 20 μmol/l px-478 before hypoxia inhibited hif-1α by 40% compared to treatment with hypoxia alone. in du 145 cells, pretreatment with 50 μmol/l px-478 before hypoxia inhibited hif-1α by 35% compared to treatment with hypoxia alone [1].in nu/nu mice with c6 reporter xenografts, treatment with px-478 at a dose of 30 mg/kg p.o. for 2 consecutive days prevented the transcriptional activity of hif-1 in central ischemic regions of c6 tumors [2].
in vivo
PX-478 is administered to mice with congenital heart disease (Nfatc1-Cre/caACVR1fl/fl) every other day starting from birth for 2 wk. Treated mice have significantly less ectopic bone at the ankle joints compared with mutant mice treated with vehicle (6.8 mm3 vs. 2.2 mm3, P<0.01)[2].
References
[1]. palayoor st, mitchell jb, cerna d, et al. px-478, an inhibitor of hypoxia-inducible factor-1α, enhances radiosensitivity of prostate carcinoma cells. international journal of cancer, 2008, 123(10): 2430-2437.
[2]. schwartz dl, powis g, thitai-kumar a, et al. the selective hypoxia inducible factor-1 inhibitor px-478 provides in vivo radiosensitization through tumor stromal effects. molecular cancer therapeutics, 2009, 8(4): 947-958.
L-Phenylalanine, 4-[bis(2-chloroethyl)oxidoaMino]-, (Hydrochloride) (1:2) Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Changzhou PBpharmaceutical R&D Co.,Ltd | 0519-83990708 | info@pbpharm.com | CHINA | 498 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22963 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| Zhengzhou Alfa Chemical Co.,Ltd | +8618530059196 | sale04@alfachem.cn | China | 12197 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24727 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
