| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
ErbBs/epidermal growth factor receptor (EGFR) exon 20 insertion mutations; BTK
(S)-Sunvozertinib targets the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), with particular potency against mutant forms including EGFR exon 20 insertions (NPH and ASV), EGFR L858R/T790M, and HER2 exon 20 YVMA insertions. It also inhibits Bruton's tyrosine kinase (BTK). As an irreversible inhibitor, it forms a covalent bond with cysteine residues in the kinase domain, providing sustained target engagement. WT EGFR is inhibited with an IC50 of 84.8 nM. |
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| ln Vitro |
(S)-Sunvozertinib inhibits WT EGFR (84.8 nM) and promotes the proliferation of Ba/F3 EGFR NPH ins (GI50=139.7 nM), Ba/F3 FGFR ASV ins (155.7 nM), NCI-HI975 EGFRL858R/T790M (24.4), and Her2 YVMA ins (827 nM)[1]. (S)-Sunvozertinib inhibits BTK WT cells (GI50 range 13.7-48 nM; OCI-LY-10, TMD-8, Ri-1, and DB) [1].
In vitro, (S)-Sunvozertinib promotes the proliferation of Ba/F3 cells expressing EGFR exon 20 NPH insertion with a GI50 of 139.7 nM, EGFR exon 20 ASV insertion with a GI50 of 155.7 nM, and EGFR L858R/T790M with an IC50 of 24.4 nM. It inhibits HER2 YVMA insertion with an IC50 of 827 nM. In BTK WT cell lines (OCI-LY-10, TMD-8, Ri-1, DB), it shows GI50 values ranging from 13.7 to 48 nM. The compound demonstrates potent and selective anti-proliferative activity against cells harboring clinically relevant EGFR mutations. |
| ln Vivo |
In vivo, (S)-Sunvozertinib is the active S-enantiomer of Sunvozertinib, which is orally bioavailable and demonstrates potent antitumor activity in preclinical models. Sunvozertinib has been granted accelerated approval by the FDA for adult patients with locally advanced or metastatic NSCLC with EGFR exon 20 insertion mutations whose disease has progressed on or after platinum-based chemotherapy. The compound shows strong inhibition of EGFR phosphorylation in tumor tissues and significant anti-tumor effects in xenograft models.
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| Enzyme Assay |
For receptor binding studies, EGFR kinase assays are performed using recombinant EGFR protein (wild-type or mutant variants) incubated with a peptide substrate and ATP in kinase buffer. The test compound is added at various concentrations (0.1-1000 nM). Kinase activity is measured using radioactive ATP incorporation or luminescent ADP detection assays. IC50 values are calculated by fitting dose-response curves. HER2 and BTK inhibition are assessed using similar biochemical assays with recombinant proteins.
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| Cell Assay |
For cell proliferation assays, Ba/F3 cells engineered to express various EGFR or HER2 mutations, or cancer cell lines such as NCI-H1975 (EGFR L858R/T790M), are seeded in 96-well plates and treated with (S)-Sunvozertinib at concentrations ranging from 0.01-10 µM for 72 hours. Cell viability is assessed using CellTiter-Glo or MTT assays. GI50 or IC50 values are calculated from dose-response curves. BTK activity is assessed in B-cell lymphoma lines such as OCI-LY-10, TMD-8, Ri-1, and DB.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice are implanted with Ba/F3 cells expressing EGFR mutations (CDX) or patient-derived NSCLC xenografts (PDX) harboring EGFR exon 20 insertions or other mutations. When tumors reach approximately 100-200 mm³, mice are randomized and treated with (S)-Sunvozertinib via oral gavage at doses determined from pharmacokinetic studies. Tumor volumes are measured twice weekly. At study endpoint, tumors are collected for Western blot analysis of EGFR phosphorylation and histopathological examination.
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| ADME/Pharmacokinetics |
(S)-Sunvozertinib is orally bioavailable and shows favorable pharmacokinetic properties suitable for once-daily oral dosing. The compound is soluble in DMSO. Storage is recommended at -20°C for long-term stability. After oral administration, it demonstrates good exposure and tissue distribution, with the ability to penetrate into tumor tissues. Further detailed PK parameters including half-life, Cmax, and AUC would be available in the primary literature and clinical data.
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| Toxicity/Toxicokinetics |
In preclinical studies, (S)-Sunvozertinib is well-tolerated at efficacious doses. The compound shows reduced activity against wild-type EGFR (IC50 = 80.4 nM in A431 cells), supporting its selectivity for mutant forms and potentially reducing on-target toxicities associated with wild-type EGFR inhibition. Comprehensive toxicology data are available from the clinical development program of Sunvozertinib, which has been FDA-approved. As a research compound, standard safety precautions should be followed.
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| References | |
| Additional Infomation |
(S)-Sunvozertinib is the S-enantiomer of Sunvozertinib (DZD-9008), a potent, selective, irreversible EGFR/HER2 inhibitor targeting exon 20 insertion mutations and other oncogenic variants. It is being developed for NSCLC with EGFR exon 20 insertions. Sunvozertinib received FDA accelerated approval on July 2, 2025. The compound inhibits EGFR L858R/T790M with IC50 of 1 nM and BTK. It is a research compound and an active pharmaceutical ingredient with clinical approval for therapeutic use in NSCLC.
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| Molecular Formula |
C29H35CLFN7O3
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|---|---|
| Molecular Weight |
584.0847
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| Exact Mass |
583.247
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| Elemental Analysis |
C, 59.63; H, 6.04; Cl, 6.07; F, 3.25; N, 16.79; O, 8.22
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| CAS # |
2370013-49-1
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| Related CAS # |
Sunvozertinib;2370013-12-8
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| PubChem CID |
139377763
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| Appearance |
White to off-white solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
41
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| Complexity |
885
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=C(C([H])=C(C(=C1[H])N([H])C1C([H])=C([H])N=C(N=1)N([H])C1=C(C([H])=C(C(=C1[H])N([H])C(C([H])=C([H])[H])=O)N1C([H])([H])C([H])([H])[C@@]([H])(C1([H])[H])N(C([H])([H])[H])C([H])([H])[H])OC([H])([H])[H])C(C([H])([H])[H])(C([H])([H])[H])O[H])F
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| InChi Key |
BTMKEDDEMKKSEF-KRWDZBQOSA-N
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| InChi Code |
InChI=1S/C29H35ClFN7O3/c1-7-27(39)34-22-14-23(25(41-6)15-24(22)38-11-9-17(16-38)37(4)5)35-28-32-10-8-26(36-28)33-21-13-19(30)20(31)12-18(21)29(2,3)40/h7-8,10,12-15,17,40H,1,9,11,16H2,2-6H3,(H,34,39)(H2,32,33,35,36)/t17-/m0/s1
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| Chemical Name |
N-[5-[[4-[5-chloro-4-fluoro-2-(2-hydroxypropan-2-yl)anilino]pyrimidin-2-yl]amino]-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]-4-methoxyphenyl]prop-2-enamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~85.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.28 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7121 mL | 8.5605 mL | 17.1209 mL | |
| 5 mM | 0.3424 mL | 1.7121 mL | 3.4242 mL | |
| 10 mM | 0.1712 mL | 0.8560 mL | 1.7121 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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