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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
Molecular Weight:
569.03
MDL Number:
MFCD28656903
MOL File:
1114544-31-8.mol
MSDS File:
SDS
Last updated:2023-09-04 15:50:00

Ponatinib Hydrochloride Properties

storage temp. -20°C
solubility DMF: 2 mg/ml,DMSO: 11 mg/ml,Ethanol: Slightly soluble
form A solid
NCI Dictionary of Cancer Terms ponatinib hydrochloride
FDA UNII 96R6PU3D8J
NCI Drug Dictionary ponatinib hydrochloride

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS08,GHS06
Signal word  Danger
Hazard statements  H302-H372-H301-H360
Precautionary statements  P260-P264-P270-P314-P501-P264-P270-P301+P312-P330-P501-P264-P270-P301+P310-P321-P330-P405-P501
NFPA 704
0
2 0

Ponatinib Hydrochloride price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Biosynth Carbosynth FP32437 Ponatinib HCl 1114544-31-8 50mg $48.5 2021-12-16 Buy
Biosynth Carbosynth FP32437 Ponatinib HCl 1114544-31-8 10mg $54 2021-12-16 Buy
AK Scientific SYN5430 Ponatinib(HClsalt) 1114544-31-8 50mg $210 2021-12-16 Buy
Crysdot CD00012996 Ponatinibhydrochloride 97% 1114544-31-8 1g $300 2021-12-16 Buy
Crysdot CD00012996 Ponatinibhydrochloride 97% 1114544-31-8 5g $950 2021-12-16 Buy
Product number Packaging Price Buy
FP32437 50mg $48.5 Buy
FP32437 10mg $54 Buy
SYN5430 50mg $210 Buy
CD00012996 1g $300 Buy
CD00012996 5g $950 Buy

Ponatinib Hydrochloride Chemical Properties,Uses,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).

Synthesis_1114544-31-8

Ponatinib Hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 101)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29919 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853 sales@tianpharm.com CHINA 304 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 967 58
Shochem(Shanghai) Co.,Ltd
86-21-50800795 info@shochem.com CHINA 288 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597 sales04@yibaibiotech.com CHINA 419 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
Hubei Ipure Biology Co., Ltd
+8613367258412 ada@ipurechemical.com China 10326 58
ANHUI WITOP BIOTECH CO., LTD
+8615255079626 eric@witopchemical.com China 23396 58

View Lastest Price from Ponatinib Hydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Ponatinib Hydrochloride pictures 2020-07-22 Ponatinib Hydrochloride
1114544-31-8
US $0.00-0.00 / KG 1g 99% 50kg/month Beijing Yibai Biotechnology Co., Ltd
Ponatinib Hydrochloride pictures 2019-09-03 Ponatinib Hydrochloride
1114544-31-8
US $1.00-2.00 / KG 1KG 95.0-99.8% 1KG;5KG 10KG; 100KG Career Henan Chemical Co

Ponatinib Hydrochloride Spectrum

AP24534 Mono-hydrochloride Ponatinib Mono-hydrochloride Ponatinib hydrochloride Ponatinib-HCl AP24534-HCl 3-(2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl)-4-methyl-n-(4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl)benzamide hydrochloride Ponatinib Hyd buscamos el HCl 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide hydrochloride Ponatinib (HCl salt) Ponatinib hydrocholoride Mercaptopurine Impurity 1-13C2,15N 1114544-31-8 C29H27F3N6OClH