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Chemical Structure| 1257628-77-5 Chemical Structure| 1257628-77-5

Structure of Olverembatinib
CAS No.: 1257628-77-5

Chemical Structure| 1257628-77-5

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GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl (WT) and Bcr-Abl (T315I) with IC50 of 0.34 and 0.68 nM, respectively.

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Product Details of Olverembatinib

CAS No. :1257628-77-5
Formula : C29H27F3N6O
M.W : 532.56
SMILES Code : O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN=C(NN=C5)C5=C4)=C3
MDL No. :MFCD26142930
InChI Key :TZKBVRDEOITLRB-UHFFFAOYSA-N
Pubchem ID :51038269

Safety of Olverembatinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Olverembatinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
ARK1 0.1 µM 24 hours Evaluate the effect of GZD824 on cell migration and invasion, results showed GZD824 significantly inhibited the migration and invasion of ARK1 cells Cancer Med. 2025 Jan;14(1):e70531
Ishikawa 0.1 µM 48 hours Evaluate the effect of GZD824 on cell migration, results showed GZD824 significantly inhibited the migration of Ishikawa cells Cancer Med. 2025 Jan;14(1):e70531
NOF 0-100 µM 72 hours Evaluate the effect of GZD824 on normal cell proliferation, results showed GZD824 had weaker inhibitory effect on NOF cells Cancer Med. 2025 Jan;14(1):e70531
HPMC 0-100 µM 72 hours Evaluate the effect of GZD824 on normal cell proliferation, results showed GZD824 had weaker inhibitory effect on HPMC cells Cancer Med. 2025 Jan;14(1):e70531
E6E7hTERT 0-100 µM 72 hours Evaluate the effect of GZD824 on normal cell proliferation, results showed GZD824 had weaker inhibitory effect on E6E7hTERT cells Cancer Med. 2025 Jan;14(1):e70531
KLE 0-100 µM 72 hours Evaluate the effect of GZD824 on cell proliferation, results showed GZD824 significantly inhibited the proliferation of KLE cells Cancer Med. 2025 Jan;14(1):e70531
RL95-2 0-100 µM 72 hours Evaluate the effect of GZD824 on cell proliferation, results showed GZD824 significantly inhibited the proliferation of RL95-2 cells Cancer Med. 2025 Jan;14(1):e70531
MFE296 0-100 µM 72 hours Evaluate the effect of GZD824 on cell proliferation, results showed GZD824 significantly inhibited the proliferation of MFE296 cells Cancer Med. 2025 Jan;14(1):e70531
HEC-1-B 0-100 µM 72 hours Evaluate the effect of GZD824 on cell proliferation, results showed GZD824 significantly inhibited the proliferation of HEC-1-B cells Cancer Med. 2025 Jan;14(1):e70531
HEC-1-A 0-100 µM 72 hours Evaluate the effect of GZD824 on cell proliferation, results showed GZD824 significantly inhibited the proliferation of HEC-1-A cells Cancer Med. 2025 Jan;14(1):e70531

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice MV-4-11 subcutaneous xenograft model Oral 10 or 30 mg/kg Every other day for 22 consecutive days HQP1351 significantly suppressed the growth of FLT3-ITD mutant AML xenograft tumors and prolonged the survival of tumor-bearing mice. Transl Oncol. 2022 Jan;15(1):101244

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05521204 Myeloproliferative Neoplasm|Ac... More >>ute Leukemia Less << PHASE2 RECRUITING 2027-08-31 First Affiliated Hospital of S... More >>oochow University, Suzhou, Jiangsu, 215000, China Less <<
NCT05594758 - AVAILABLE - -
NCT05931757 Philadelphia-Positive ALL PHASE2 NOT_YET_RECRUITING 2030-06-30 First Affiliated Hospital of S... More >>oochow University, Suzhou, Jiangsu, 215000, China Less <<
NCT06640361 GIST PHASE3 RECRUITING 2029-06-30 Sun Yat-sen University Cancer ... More >>Center, Guangzhou, Guangdong, 510000, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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