Ponatinib Hydrochloride
- Product Name
- Ponatinib Hydrochloride
- CAS No.
- 1114544-31-8
- Chemical Name
- Ponatinib Hydrochloride
- Synonyms
- 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide hydrochloride;AP24534-HCl;Ponatinib-HCl;Ponatinib Hyd;buscamos el HCl;Ponatinib (HCl salt);Ponatinib hydrochloride;Ponatinib hydrocholoride;AP24534 Mono-hydrochloride;Ponatinib Mono-hydrochloride
- CBNumber
- CB52657391
- Molecular Formula
- C29H28ClF3N6O
- Formula Weight
- 569.03
- MOL File
- 1114544-31-8.mol
Ponatinib Hydrochloride Property
- storage temp.
- -20°C
- solubility
- DMF: 2 mg/ml,DMSO: 11 mg/ml,Ethanol: Slightly soluble
- form
- A solid
- color
- Off-white to light yellow
- InChI
- InChI=1S/C29H27F3N6O.ClH/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37;/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39);1H
- InChIKey
- BWTNNZPNKQIADY-UHFFFAOYSA-N
- SMILES
- C(C1=CN=C2C=CC=NN12)#CC1C(=CC=C(C(=O)NC2C=CC(CN3CCN(C)CC3)=C(C(F)(F)F)C=2)C=1)C.Cl
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H302Harmful if swallowed
H360May damage fertility or the unborn child
H372Causes damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P314Get medical advice/attention if you feel unwell.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- FP32437
- Product name
- Ponatinib HCl
- Packaging
- 50mg
- Price
- $48.5
- Updated
- 2021/12/16
- Product number
- FP32437
- Product name
- Ponatinib HCl
- Packaging
- 10mg
- Price
- $54
- Updated
- 2021/12/16
- Product number
- SYN5430
- Product name
- Ponatinib(HClsalt)
- Packaging
- 50mg
- Price
- $210
- Updated
- 2021/12/16
- Product number
- CD00012996
- Product name
- Ponatinibhydrochloride
- Purity
- 97%
- Packaging
- 1g
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CD00012996
- Product name
- Ponatinibhydrochloride
- Purity
- 97%
- Packaging
- 5g
- Price
- $950
- Updated
- 2021/12/16
Ponatinib Hydrochloride Chemical Properties,Usage,Production
Description
In December 2012, the US FDA approved ponatinib (also referred to as AP 24534) for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronicmyeloid leukemia (CML). Ponatinib is a pan-Bcr–Abl TKI that blocks both the native (IC50=0.4 nM) and Bcr– AblT315I mutated kinases (IC50=2.0 nM) in addition to othermutated kinases in CML patients. In the Ba/F3 cell proliferation assay, ponatinib inhibits ABL and the T315I Abl mutant with IC50s of 1.2 and 8.8 nM, respectively. Ponatinib was identified by a structure-based drug design approach. Ponatinib binds to the kinase domain in a DFG-out conformation; the ethynyl moiety helps the inhibitor evade the mutant gatekeeper isoleucine residue at position 315. In addition to Abl and the T315I mutant of Abl, ponatinib inhibits VEGFR, PDGFR, FGFR, SRC, KIT, RET, TIE2, FLT3, and EPH receptors at concentrations ranging from0.1 to 20 nM.
Originator
Ariad (United States)
Uses
Ponatinib is a tyrosine kinase inhibitors (TKI) and used to treat chronic myeloid leukemia (CML) (1,2,3). Ponatinib is also used in combination with other drugs, such as forskolin, to combat TKI resistance in patient with CML (3), targeted drug in small-cell lung cancer. Potent FAK inhibitor. FGFR/VEGFR/Bcr-Abl inhibitor It is a COVID19-related research product.
Definition
ChEBI: Ponatinib hydrochloride is the hydrochloride salt of ponatinib. It is a potent pan inhibitor of tyrosine kinases, active in all single resistance ABL kinase mutations including the T315l mutation. It is approved for the treatment of chronic myeloid leukemia. It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It contains a ponatinib(1+).
brand name
Iclusig
Clinical Use
Ponatinib hydrochloride (Iclusig ®), previously known as AP24534, is a multi-targeted tyrosine kinase inhibitor approved in the US as an oral treatment for resistant or intolerant chronic myeloid leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). Ponatinib hydrochloride was designed for treatment of tumors containing the T351I mutation which are present in some forms of CML and resistant to traditional therapies such as imatinib. Ponatinib hydrochloride was developed by Ariad Pharmaceauticals, and operates by a similar mechanism of action as other tyrosine kinase inhibitors, inhibiting the enzymatic activity of BCR-ABL, an abnormal tyrosine kinase responsible for unregulated and excess white blood cell production by bone marrow. However, the ability of ponatinib hydrochloride to target isoforms of the BCR-ABL gene typically leading to resistance in other known tyrosine kinase inhibitors provides an alternate form of therapy not previously available.
Synthesis
A significant amount of research has been devoted towards identification of a manufacturing synthesis of ponatinib hydrochloride. A majority of methods rely on two key Sonagashira couplings to generate the imidazo[1,2-b]pyridazin-3-ylethynyl framework. The most likely process scale method begins with 3-bromo-imidazo[1,2-b]pyridazine (135) (the Scheme). Direct Sonogashira coupling of (135) with ethynyltrimethylsilane (136) in the presence of Pd(PPh3)4 and CuI, followed by treatment with TBAF/THF led to the desired alkynyl imidazo[1,2-b]pyridazine 138 in 71 and 94% yields, respectively. Alkyne 138 was then coupled under similar Sonogashira conditions with functionalized aryl iodide 139 (generated in two steps from 3-iodo-4-methylbenzoic acid (140) and commercially available piperazinyl aniline 141) providing ponatinib free base, which was then immediately treated with EtOH/HCl at room temperature to ultimately furnish ponatinib hydrochloride (XXI).
Ponatinib Hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Ponatinib Hydrochloride manufacturers
- Product
- Ponatinib Hydrochloride 1114544-31-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-24
- Product
- Ponatinib Hydrochloride 1114544-31-8
- Price
- US $0.00-0.00/KG
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 50kg/month
- Release date
- 2019-08-16
- Product
- Ponatinib Hydrochloride 1114544-31-8
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 95.0-99.8%
- Supply Ability
- 1KG;5KG 10KG; 100KG
- Release date
- 2019-09-02