BH-30643 is a novel, orally available, non-covalent, macrocyclic, mutant selective OMNI-EGFR inhibitor that targets a broad diversity of mutations in the EGFR kinase domain. These include EGFR classical mutations (e.g., ex19del and L858R) as well as less common (atypical) mutations (including G719X, S768I, L861Q, E709X, and beyond). BH-30643 also overcomes a variety of mutations which can cause resistance to previously approved EGFR TKIs (including both C797S and T790M). BH-30643 was designed to be selective over wildtype EGFR and HER2.
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| Name | BH-30643 |
|---|---|
| Iupac Chemical Name | (S)-2-((S,E)-53-ethoxy-11,13,27,7,9-pentamethyl-11H,21H,51H-10-oxa-7-aza-2(5,3)-pyrazolo[3,4-c]pyridina-1,5(4,5)-dipyrazolacyclodecaphan-3-en-51-yl)propan-1-ol |
| Synonyms | BH30643; BH-30643; BH 30643 |
| Molecular Formula | C27H36N8O3 |
| Molecular Weight | 520.6 |
| Smile | CC1=NC2=CC3=C1NN=C3/C=C/C(C(OCC)=NN4[C@@H](C)CO)=C4CN(C)C[C@H](C)OC5=C2C(C)=NN5C |
| InChiKey | IBMIIAILYKKSRC-IGXNXKSNSA-N |
| InChi | InChI=1S/C27H36N8O3/c1-8-37-26-19-9-10-21-20-11-22(28-18(5)25(20)30-29-21)24-17(4)31-34(7)27(24)38-16(3)12-33(6)13-23(19)35(32-26)15(2)14-36/h9-11,15-16,36H,8,12-14H2,1-7H3,(H,29,30)/b10-9+/t15-,16-/m0/s1 |
| CAS Number | 3062177-59-4 |
| Related CAS | 3062177-59-4 |
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| 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 (DMSO : ≥ 100 mg/mL) |
| 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 | OMNI-EGFR inhibitor |
|---|---|
| Mechanism | BH-30643 is a non-covalent, reversible inhibitor designed to target the active conformation of the EGFR/HER2 kinases. By largely sparing wild-type (normal) EGFR, it aims to reduce common side effects like skin rashes. |
| Cell study | |
| Animal study | |
| Clinical study | BH-30643 is currently being evaluated in the multi-center Phase 1/2 SOLARA trial (ClinicalTrials.gov ID: NCT06706076). This study is designed to evaluate its safety, optimal dosing, and anti-tumor efficacy in adult patients who have locally advanced or metastatic NSCLC. |