STX-478
STX-478 is an allosteric PI3Kα inhibitor that selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor xenografts without causing the metabolic dysfunction observed with alpelisib. Combining STX-478 with fulvestrant and/or cyclin-dependent kinase 4/6 inhibitors was well tolerated and provided robust and durable tumor regression in ER+HER2− xenograft tumor models.
For research use only. We do not sell to patients.
Chemical Information
| Name | STX-478 |
|---|---|
| Iupac Chemical Name | (R)-1-(2-aminopyrimidin-5-yl)-3-(1-(5,7-difluoro-3-methylbenzofuran-2-yl)-2,2,2-trifluoroethyl)urea |
| Synonyms | STX-478; STX 478; STX478; |
| Molecular Formula | C16H12F5N5O2 |
| Molecular Weight | 401.29 |
| Smile | NC1=NC=C(C=N1)NC(N[C@H](C2=C(C3=CC(F)=CC(F)=C3O2)C)C(F)(F)F)=O |
| InChiKey | LGPNQALKGDDVBD-CYBMUJFWSA-N |
| InChi | InChI=1S/C16H12F5N5O2/c1-6-9-2-7(17)3-10(18)12(9)28-11(6)13(16(19,20)21)26-15(27)25-8-4-23-14(22)24-5-8/h2-5,13H,1H3,(H2,22,23,24)(H2,25,26,27)/t13-/m1/s1 |
| CAS Number | 2883540-92-7 |
| Related CAS | 2883540-92-7 |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | ≧98.0% |
| 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. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Kearney AL, Vasan N. A New Wave of PI3Kα Inhibitors. Cancer Discov. 2023 Nov 1;13(11):2313-2315. doi: 10.1158/2159-8290.CD-23-0945. PMID: 37909093.
2: Buckbinder L, St Jean DJ Jr, Tieu T, Ladd B, Hilbert B, Wang W, Alltucker JT, Manimala S, Kryukov GV, Brooijmans N, Dowdell G, Jonsson P, Huff M, Guzman-Perez A, Jackson EL, Goncalves MD, Stuart DD. STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts. Cancer Discov. 2023 Nov 1;13(11):2432-2447. doi: 10.1158/2159-8290.CD-23-0396. PMID: 37623743; PMCID: PMC10618743.
Chemical Structure
