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Chemical Structure| 1353550-13-6 Chemical Structure| 1353550-13-6

Structure of Olmutinib
CAS No.: 1353550-13-6

Chemical Structure| 1353550-13-6

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Olmutinib inhibits EGFR with IC50 values of 9.2 nM and 10 nM in HCC827 (expressing EGFR-del 19) and H1975 (expressing EGFR-L858R/T790M) cell respectively. It is a new targeted drug for the treatment of mutation-positive NSCLC.

Synonyms: HM61713, BI 1482694; HM61713; BI 1482694

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Product Details of Olmutinib

CAS No. :1353550-13-6
Formula : C26H26N6O2S
M.W : 486.59
SMILES Code : C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
Synonyms :
HM61713, BI 1482694; HM61713; BI 1482694
MDL No. :MFCD29918158
InChI Key :FDMQDKQUTRLUBU-UHFFFAOYSA-N
Pubchem ID :54758501

Safety of Olmutinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Olmutinib

RTK
JAK-STAT

Isoform Comparison

Biological Activity

Description
Olmutinib (HM61713; BI-1482694) is an orally administered, irreversible inhibitor of the EGFR tyrosine kinase, specifically designed to bind to a cysteine residue close to the kinase domain. It is primarily used in the treatment of non-small cell lung cancer (NSCLC)[1].[2].
Target
  • EGFR/ErbB1

In Vitro:

Cell Line
Concentration Treated Time Description References
KB-CV60 3 μM 72 hours Did not significantly reverse ABCC1-mediated multidrug resistance PMC6189370
KB-C2 3 μM 72 hours Did not significantly reverse ABCB1-mediated multidrug resistance PMC6189370
YU-1089 cells 1 μM 24 hours Evaluated the effect of olmutinib in combination with tozasertib, showing that the combination significantly inhibited cell growth and increased expression of apoptotic markers. PMC6934824
Calu-3 cells 9.76 μM (IC50) 48 hours Evaluate the inhibitory effect of Olmutinib on SARS-CoV-2 infection, results showed an IC50 of 9.76 μM but exhibited substantial cell toxicity. PMC10275482
HEK293/ABCG2–482-T7 1 μM 72 hours Olmutinib significantly reduced the IC50 values of MX in HEK293/ABCG2–482-T7 cells PMC6089862
HEK293/ABCG2–482-R2 1 μM 72 hours Olmutinib significantly reduced the IC50 values of MX in HEK293/ABCG2–482-R2 cells PMC6089862
S1-MI-80 1 μM 72 hours Olmutinib significantly enhanced the sensitivity of ABCG2-overexpressing S1-MI-80 cells to MX and topotecan PMC6089862
H460/MX20 1 μM 72 hours Olmutinib significantly enhanced the sensitivity of ABCG2-overexpressing H460/MX20 cells to MX and topotecan PMC6089862
NCI-H460/MX20 3 μM 72 hours Reversed ABCG2-mediated multidrug resistance by antagonizing the drug efflux function in ABCG2-overexpressing cells PMC6189370

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice (BALB/c-nude) S1-MI-80 cell xenograft model Oral 30 mg/kg Every 5 days for 75 days Olmutinib significantly enhanced the inhibitory effect of topotecan on the growth of S1-MI-80 xenograft tumors, with an inhibition rate of 65% PMC6089862
Mice Thioacetamide-induced liver and kidney toxicity model Oral 30 mg/kg Once daily for five days To evaluate the effect of Olmutinib on thioacetamide-induced liver and kidney toxicity. Results showed that Olmutinib potentiated TAA-induced toxicity. PMC9228264

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02444819 Non Small Cell Lung Cancer PHASE2 COMPLETED 2025-08-17 Seoul, Korea, Republic of
NCT03228277 Non Small Cell Lung Cancer PHASE2 COMPLETED 2019-07-31 Konkuk University Medical Cent... More >>er, Seoul, 05030, Korea, Republic of Less <<
NCT02485652 Non Small Cell Lung Cancer PHASE2 TERMINATED 2020-12-08 Research Site, Beverly Hills, ... More >>California, United States|Research Site, Burbank, California, United States|Research Site 2, Los Angeles, California, United States|Research Site, Los Angeles, California, United States|Research Site, Montebello, California, United States|Research Site, Orange, California, United States|Research Site, San Diego, California, United States|Research Site, Boca Raton, Florida, United States|Research Site, Honolulu, Hawaii, United States|Research Site, Evanston, Illinois, United States|Research Site, Bethesda, Maryland, United States|Research Site, Boston, Massachusetts, United States|Research Site, Lebanon, New Hampshire, United States|Research Site, Charlotte, North Carolina, United States|Research Site, Washington, Washington, United States|Research Site, Darlinghurst, Australia|Research site, Fitzroy, Australia|Research Site, Frankston, Australia|Research Site, Kogarah, Australia|Research Site, St Albans, Australia|Research Site, Woolloongabba, Australia|Research Site, Toronto, Canada|Research Site, Berlin, Germany|Research Site, Homburg, Germany|Research Site, Leipzig, Germany|Research Site, München, Germany|Research Site, Ulm, Germany|Research Site, Bergamo, Italy|Research Site, Bologna, Italy|Research Site, Catania, Italy|Research Site, Milano, Italy|Research Site, Rome, Italy|Research Site, Cheongju-si, Korea, Republic of|Research Site, Goyang-si, Korea, Republic of|Research Site, Hwasun, Korea, Republic of|Research Site, Incheon, Korea, Republic of|Research Site 2, Seongnam-si, Korea, Republic of|Research Site, Seongnam-si, Korea, Republic of|Research Site 2, Seoul, Korea, Republic of|Research Site 3, Seoul, Korea, Republic of|Research Site 4, Seoul, Korea, Republic of|Research Site 5, Seoul, Korea, Republic of|Research Site 6, Seoul, Korea, Republic of|Research Site 7, Seoul, Korea, Republic of|Research Site 8, Seoul, Korea, Republic of|Research Site, Seoul, Korea, Republic of|Research Site, George Town, Penang, Malaysia|Research Site, Kuala Lumpur, Malaysia|Research Site, Kuantan, Malaysia|Research Site, Kuching, Malaysia|Research Site, Makati, Kalakhang Maynila, Philippines|Research Site, Pasig, Manila, Philippines|Research Site 2, Manila, Metro Manila, Philippines|Research Site, Manila, Metro Manila, Philippines|Research Site, Cebu, Philippines|Research Site 2, Barcelona, Spain|Research Site 3, Barcelona, Spain|Research Site 4, Barcelona, Spain|Research Site, Barcelona, Spain|Research Site, La Coruna, Spain|Research Site 2, Madrid, Spain|Research Site, Madrid, Spain|Research Site, Navarra, Spain|Research Site, San Sebastian, Spain|Research Site 2, Valencia, Spain|Research Site, Valencia, Spain|Research Site, Kaohsiung, Taiwan|Research Site, Taichung, Taiwan|Research Site 2, Tainan, Taiwan|Research Site, Tainan, Taiwan|Research Site 2, Taipei, Taiwan|Research Site, Taipei, Taiwan Less <<
NCT04510415 Non Small Cell Lung Cancer PHASE1 TERMINATED 2018-12-11 National Cancer Center, Gyeong... More >>gi-do, Korea, Republic of|The Catholic Univ. of Korea Bucheon St.Mary's Hospital, Gyeonggi-do, Korea, Republic of|The Catholic Univ. of Korea St.Vincent's Hospital, Gyeonggi-do, Korea, Republic of|The Catholic Univ. of Korea Uijeongbu St.Mary's Hospital, Gyeonggi-do, Korea, Republic of|Gachon University Gil Medical Center, Incheon, Korea, Republic of|The Catholic Univ. of Korea Incheon St.Mary's Hospital, Incheon, Korea, Republic of|Samsung Medical Center, Seoul, Korea, Republic of|The Catholic Univ. of Korea Seoul St.Mary's Hospital, Seoul, Korea, Republic of Less <<
NCT01894399 Healthy Volunteers PHASE1 COMPLETED 2025-11-13 Research Site, Seoul, Korea, R... More >>epublic of Less <<
NCT01588145 Non Small Cell Lung Cancer PHASE1|PHASE2 COMPLETED 2025-08-17 Seoul, Korea, Republic of

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.28mL

2.06mL

1.03mL

20.55mL

4.11mL

2.06mL

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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