ChemicalBook > CAS DataBase List > Olverembatinib

Olverembatinib

Product Name: Olverembatinib
CAS No.: 1257628-77-5
Chemical Name: Olverembatinib
Synonyms: GZD824;GZD8824;GZD-824;GZD 824;GZD-824 Free;Olverembatinib;GZD 824 USP/EP/BP;GZD824;GZD-824;GZD 824;Olverembatinib (GZD824);GZD-824; GZD 824;BENZAMIDE
CBNumber: CB82666626
Molecular Formula: C29H27F3N6O
Formula Weight: 532.56
MOL File: 1257628-77-5.mol

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Olverembatinib Property

Boiling point:: 630.4±55.0 °C(Predicted)
Density: 1.39±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : ≥ 100 mg/mL (187.77 mM)
form: A crystalline solid
pka: 9.04±0.40(Predicted)
color: Off-white to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 21508
Product name: GZD-824
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 21508
Product name: GZD-824
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 21508
Product name: GZD-824
Purity: ≥98%
Packaging: 10mg
Price: $243
Updated: 2024/03/01

Cayman Chemical

Product number: 21508
Product name: GZD-824
Purity: ≥98%
Packaging: 25mg
Price: $456
Updated: 2024/03/01

TRC

Product number: G932028
Product name: GZD824
Packaging: 10mg
Price: $195
Updated: 2021/12/16

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Olverembatinib Chemical Properties,Usage,Production

Description

GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC₅₀s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/Abl^T315I, respectively). It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC₅₀s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.

Uses

GZD824 is a orally bioavailable inhibitor that targets phosphorylated and non-phosphorylated Breakpoint Cluster Region-Abelson (Bcr-Abl) kinases. It is a COVID19-related research product.

Definition

GZD 824 (Olverembatinib), another third-generation BCR-ABL tyrosine kinase inhibitor (TKI), was approved in 2021 in China for patients with T315I positive chronic phase chronic myeloid leukemia (CML-CP) or accelerated-phase CML (CML-AP). Like ponatinib, olverembatinib inhibits multikinases, including B-RAF, DDR1, FGFR, Flt3, KIT, PDGFRα/β, RET, and SRC.

Application

Olverembatinib is able to inhibit wild-type BCR-ABL1 kinase and a wide range of related mutants, including the T315I mutant, which makes it a potential treatment for TKI-resistant CML patients. In addition, Olverembatinib is also being studied for the treatment of acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL) and solid tumors.

General Description

Class: non-receptor tyrosine kinase
Treatment: CML
Elimination half-life = 17.5–36.5 h

Synthesis

In a recent patent, the synthesis of olverembatinib began with a Sonogashira coupling reaction of commercially available alkyne 24.1 with pyridinium bromide 24.2 to afford ester 24.3 in 98% yield. The N-Boc group of carbonate 24.3 was cleaved by refluxing in a mixture of MeOH and water to afford pyrazole 24.4 in 91% yield. Finally, potassium tert-butoxide-mediated amide formation with aniline 24.5 afforded olverembatinib (24) in 88% yield.

target

BCR-ABL

References

[1] XIAOMEI REN. Identification of GZD824 as an Orally Bioavailable Inhibitor That Targets Phosphorylated and Nonphosphorylated Breakpoint Cluster Region–Abelson (Bcr-Abl) Kinase and Overcomes Clinically Acquired Mutation-Induced Resistance against Imatinib[J]. Journal of Medicinal Chemistry, 2013, 56 3: 879-894. DOI: 10.1021/jm301581y

Olverembatinib Preparation Products And Raw materials

Raw materials

Preparation Products

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1257628-77-5, OlverembatinibRelated Search:

Actin from Rabbit Muscle NS-398 Nilotinib hydrochloride anhydrous Axitinib Cabozantinib Palbociclib Trametinib Dacomitinib (PF299804) Lenvatinib Tofacitinib

GZD-824; GZD 824;BENZAMIDE

4-Methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]benzamide

3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide

GZD8824

GZD824;GZD-824;GZD 824

GZD-824 Free

GZD 824

GZD824

GZD-824

Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-

GZD 824 USP/EP/BP

3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide

Olverembatinib

Olverembatinib (GZD824)

3-[(1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]benzamide

4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-3-(2-{1H-pyrazolo[3,4-b]pyridin-5-yl}ethynyl)benzamide

Olverembatinib, 10 mM in DMSO

1257628-77-5

257628-77-5

Inhibitors