- Olverembatinib
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- $30.00
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2026-07-27
- CAS:1257628-77-5
- Purity: 98.64%
- Supply Ability: 10g
- Olverembatinib
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2026-07-25
- CAS:1257628-77-5
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 1000kgs
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| | Olverembatinib Basic information |
| Product Name: | Olverembatinib | | Synonyms: | 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;Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]- | | CAS: | 1257628-77-5 | | MF: | C29H27F3N6O | | MW: | 532.56 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1257628-77-5.mol |  |
| | Olverembatinib Chemical Properties |
| 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 |
| | Olverembatinib Usage And Synthesis |
| 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/AblT315I, 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 |
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