CB-103 is a γ-secretase inhibitor. CB-103 inhibits Notch signaling in primary human T cell acute lymphoblastic leukemia and other Notch-dependent human tumor cell lines, and concomitantly induces cell cycle arrest and apoptosis, thereby impairing proliferation, including in GSI-resistant human tumor cell lines with chromosomal translocations and rearrangements in Notch genes. CB-103 produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts, notably without causing the dose-limiting intestinal toxicity associated with other Notch inhibitors.
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Name | CB-103 |
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Iupac Chemical Name | 5-Amino-2-(4-tert-butylphenoxy)pyridine |
Synonyms | CB-103; CB 103; CB103; |
Molecular Formula | C15H18N2O |
Molecular Weight | 242.32 |
Smile | CC(C)(C)C1=CC=C(C=C1)OC2=NC=C(C=C2)N |
InChiKey | WHIWGRCYMQLLAO-UHFFFAOYSA-N |
InChi | InChI=1S/C15H18N2O/c1-15(2,3)11-4-7-13(8-5-11)18-14-9-6-12(16)10-17-14/h4-10H,16H2,1-3H3 |
CAS Number | 218457-67-1 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | Solid powder |
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Purity | 98% Min. |
Storage | 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 |
Handling | |
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. |
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Clinical study |
1: Fabbro D, Bauer M, Murone M, Lehal R. Notch Inhibition in Cancer: Challenges and Opportunities. Chimia (Aarau). 2020 Oct 28;74(10):779-783. doi: 10.2533/chimia.2020.779. PMID: 33115560.
2: Lehal R, Zaric J, Vigolo M, Urech C, Frismantas V, Zangger N, Cao L, Berger A, Chicote I, Loubéry S, Choi SH, Koch U, Blacklow SC, Palmer HG, Bornhauser B, González-Gaitán M, Arsenijevic Y, Zoete V, Aster JC, Bourquin JP, Radtke F. Pharmacological disruption of the Notch transcription factor complex. Proc Natl Acad Sci U S A. 2020 Jul 14;117(28):16292-16301. doi: 10.1073/pnas.1922606117. Epub 2020 Jun 29. PMID: 32601208; PMCID: PMC7368267.