| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Sunvozertinib's GI50 values were 60.4, 83.2, 3.3, 101.3, and 47.1 nM A431, respectively, against the EGFR exon NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, Her2 Exon20 YVMA, and EGFR WT. For BTK WT OCI -LY-10, BTK WT TMD-8, BTK WT Ri-1, and non-BCR activated DB, the GI50 of sunvozertinib was 3.2, 5.8, 51.3, and 1983.5 nM, respectively [1]. p-BTK is inhibited by sunvozertinib at an IC50 of 1.6 nM[1].
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| References | |
| Additional Infomation |
Sunvozertinib is an orally available, irreversible, dual kinase inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) that shows similar activity against certain activating mutations, including exon 20 insertions (exon20ins), with potential antineoplastic activity. Upon oral administration,sunvozertinib binds to and inhibits EGFR and HER2, which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization. In contrast to other agents active against exon20ins mutations, sunvozertinib appears to be more selective against mutated EGFR than wild-type (wt) EGFR. This may lessen wtEGFR-related dose-limiting toxicity and may allow for the administration of the desired therapeutic dose of sunvozertinib.
Drug Indication Treatment of non-small cell lung cancer |
| Molecular Formula |
C29H35CLFN7O3
|
|---|---|
| Molecular Weight |
584.084708452225
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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 # |
2370013-12-8
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| Related CAS # |
(S)-Sunvozertinib;2370013-49-1
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| PubChem CID |
139377809
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| Appearance |
Off-white to light brown 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 |
CC(C)(C1=CC(=C(C=C1NC2=NC(=NC=C2)NC3=C(C=C(C(=C3)NC(=O)C=C)N4CC[C@H](C4)N(C)C)OC)Cl)F)O
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| InChi Key |
BTMKEDDEMKKSEF-QGZVFWFLSA-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-/m1/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-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]-4-methoxyphenyl}prop-2-enamide
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| Synonyms |
DZD-9008Sunvozertinib DZD 9008 DZD9008
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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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