Zotizalkib ( TPX-0131 )
TPX-0131 is a next-generation ALK inhibitor drug candidate currently being evaluated in our Phase 1/2 FORGE-1 clinical trial of patients with ALK+ advanced non-small lung cancer (NSCLC). It has been designed with a novel compact macrocyclic structure and has shown preclinical potent inhibition of wildtype and numerous ALK mutations, including the clinically observed G1202R solvent-front mutation and the G1202R/L1196M compound mutation.
For research use only. We do not sell to patients.
Chemical Information
| Name | Zotizalkib ( TPX-0131 ) |
|---|---|
| Iupac Chemical Name | (S,14aE,15aE)-13-(difluoromethyl)-35-fluoro-6,6-dimethyl-13,14-dihydro-12H-4-oxa-7-aza-1(4,6)-pyrazolo[1',5':1,2]pyrimido[5,4-b][1,4]oxazina-3(1,2)-benzenacyclooctaphan-8-one |
| Synonyms | Zotizalkib ; TPX-0131 ; TPX 0131 ; TPX0131 ; |
| Molecular Formula | C21H20F3N5O3 |
| Molecular Weight | 447.41 |
| Smile | FC([C@H]1N2C3=NC4=C(C(NC(C)(COC5=CC=C(F)C=C5C2)C)=O)C=NN4C=C3OC1)F |
| InChiKey | ILAMRXVQSGVCJX-AWEZNQCLSA-N |
| InChi | InChI=1S/C21H20F3N5O3/c1-21(2)10-32-15-4-3-12(22)5-11(15)7-28-14(17(23)24)9-31-16-8-29-18(26-19(16)28)13(6-25-29)20(30)27-21/h3-6,8,14,17H,7,9-10H2,1-2H3,(H,27,30)/t14-/m0/s1 |
| CAS Number | 2648641-36-3 |
| Related CAS | 2648641-36-3 |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | ≧98.0% |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | Refer to MSDS |
| 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. |
| HS Code | 2934200090 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Ou SI, Nagasaka M, Brazel D, Hou Y, Zhu VW. Will the clinical development of 4th-generation "double mutant active" ALK TKIs (TPX-0131 and NVL-655) change the future treatment paradigm of ALK+ NSCLC? Transl Oncol. 2021 Nov;14(11):101191. doi: 10.1016/j.tranon.2021.101191. Epub 2021 Aug 5. PMID: 34365220; PMCID: PMC8353359.
2: Murray BW, Zhai D, Deng W, Zhang X, Ung J, Nguyen V, Zhang H, Barrera M, Parra A, Cowell J, Lee DJ, Aloysius H, Rogers E. TPX-0131, a Potent CNS- penetrant, Next-generation Inhibitor of Wild-type ALK and ALK-resistant Mutations. Mol Cancer Ther. 2021 Sep;20(9):1499-1507. doi: 10.1158/1535-7163.MCT-21-0221. Epub 2021 Jun 22. PMID: 34158340.
Chemical Structure
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