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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
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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
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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..…

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N-Bromosuccinimide Price

Biosynth Carbosynth
Product number
FP32437
Product name
Ponatinib HCl
Packaging
50mg
Price
$48.5
Updated
2021/12/16
Biosynth Carbosynth
Product number
FP32437
Product name
Ponatinib HCl
Packaging
10mg
Price
$54
Updated
2021/12/16
AK Scientific
Product number
SYN5430
Product name
Ponatinib(HClsalt)
Packaging
50mg
Price
$210
Updated
2021/12/16
Crysdot
Product number
CD00012996
Product name
Ponatinibhydrochloride
Purity
97%
Packaging
1g
Price
$300
Updated
2021/12/16
Crysdot
Product number
CD00012996
Product name
Ponatinibhydrochloride
Purity
97%
Packaging
5g
Price
$950
Updated
2021/12/16
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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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Ponatinib Hydrochloride Suppliers

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View Lastest Price from Ponatinib Hydrochloride manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
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
Beijing Yibai Biotechnology Co., Ltd
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
Career Henan Chemical Co
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

1114544-31-8, Ponatinib HydrochlorideRelated Search:


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