Olverembatinib (GZD824)
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MedKoo CAT#: 407111

CAS#: 1257628-77-5

Description: Olverembatinib, also known as GZD824, is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. GZD824 tightly bound to Bcr-Abl(WT) and Bcr-Abl(T315I) with K(d) values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase functions with nanomolar IC(50) values. GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. GZD824 also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy. It induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I). GZD824 represents a promising lead candidate for development of Bcr-Abl inhibitors to overcome acquired imatinib resistance. (J Med Chem. 2013 Feb 14;56(3):879-94)


Price and Availability

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 850 Same day
500mg USD 1850 Same day
1g USD 3250 Same day
2g USD 4250 Same day
5g USD 6950 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-28. Prices are subject to change without notice.

Olverembatinib (GZD824), purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407111
Name: Olverembatinib (GZD824)
CAS#: 1257628-77-5
Chemical Formula: C29H27F3N6O
Exact Mass: 532.21984
Molecular Weight: 532.22
Elemental Analysis: C, 65.40; H, 5.11; F, 10.70; N, 15.78; O, 3.00


Related CAS #: 1257628-77-5    

Synonym: GZD824; GZD 824; GZD-824; Olverembatinib;

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

InChi Key: TZKBVRDEOITLRB-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H27F3N6O/c1-19-3-5-22(14-21(19)6-4-20-13-24-17-34-36-27(24)33-16-20)28(39)35-25-8-7-23(26(15-25)29(30,31)32)18-38-11-9-37(2)10-12-38/h3,5,7-8,13-17H,9-12,18H2,1-2H3,(H,35,39)(H,33,34,36)

SMILES Code: CC1=CC=C(C=C1C#CC2=CN=C3C(C=NN3)=C2)C(NC4=CC=C(C(C(F)(F)F)=C4)CN5CCN(CC5)C)=O


Technical Data

Appearance:
White to off-white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y, Zhuang X, Zhang F, Liu J, Leng F, Lang X, Bai Y, She M, Tu Z, Pan J, Ding K. 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 Med Chem. 2013 Feb 14;56(3):879-94. doi: 10.1021/jm301581y. Epub 2013 Jan 28. PubMed PMID: 23301703.