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TQB-3804 (TQB3804; EGFR-IN-7; compound 34) is a 4th-generation, oralli bioactive and selective EGFR kinase inhibitor (EGFR-TKI, developed in China and disclosed in patent WO2019015655A1) with potential anticancer activity. It inhibits EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50s of 7.92 nM and 0.218 nM, respectively.
| ln Vitro |
For EGFR (WT), EGFR (Δ19del/T790M/C797S), and EGFR (C797S/T790M/L858R), EGFR-IN-7 (10 mM) exhibits a potent inhibitory effect on their respective enzymatic activities, with IC50 values of 7.92 nM, 0.218 nM, and 0.16 nM, respectively[1]. As demonstrated by its IC50 value of 154 nM, EGFR-IN-7 (1 mM) exhibits good selectivity for EGFR (WT) in A431 cells. The Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant cells are well-inhibited by EGFR-IN-7 (10 μM-0.508 nM), with an IC50 value of 22 nM[1]. For pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells, EGFR-IN-7 (10 μM or 100 μM) suppresses phosphorylation activity with an IC50 value of 19 nM[1].
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| ln Vivo |
EGFR-IN-7 (Compound 34; 5-45 mg/kg; oral; daily; for 13 days) exhibited in Ba/F 3 (Δ19del/T790M/C797S)-derived xenografts (CDX) implanted subcutaneously Effective anti-tumor activity) BALB/c nude mouse drug resistance model [1]. EGFR-IN-7 (25 and 50 mg/kg; oral; daily for 3 weeks) effectively reduces tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model [1].
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| Cell Assay |
Cell proliferation experiment [1]
Cell Types: A431 cells; Ba/F 3 (EGFRΔ19del/T790M/C797S) Suspension cell Tested Concentrations: 1 mM; 10 μM-0.508 nM Incubation Duration: 3 days Experimental Results: Inhibited cell proliferation. |
| Animal Protocol |
Animal/Disease Models: Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g) [1] Doses: 5, 15, 45 mg/kg
Route of Administration: Orally, one time/day, for 13 days. Experimental Results: The half-life, plasma and tissue exposure were Dramatically increased, and it had good pharmacokinetic/PK/PK effects in mice. Animal/Disease Models: subcutaneousxenograft PC-9 (Δ19del) model [1] Doses: Days 0-9: 50 mg/kg, Days 10-21: 25 mg/kg Route of Administration: Orally, one time/day, 3 weeks Experimental Results: It has a significant inhibitory effect on tumor growth, has a tumor reducing effect, and shows good anti-tumor efficacy. |
| References |
| Molecular Formula |
C32H41BRN9O2P
|
|---|---|
| Molecular Weight |
694.6048
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| Exact Mass |
693.23
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| Elemental Analysis |
C, 55.33; H, 5.95; Br, 11.50; N, 18.15; O, 4.61; P, 4.46
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| CAS # |
2267329-76-8
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| Related CAS # |
2267329-76-8;
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| PubChem CID |
138911391
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
45
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| Complexity |
994
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZYSKXRAGBGLELB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H41BrN9O2P/c1-21-18-26(28(44-3)19-27(21)42-12-8-22(9-13-42)41-16-14-40(2)15-17-41)38-32-36-20-23(33)31(39-32)37-25-7-6-24-29(35-11-10-34-24)30(25)45(4,5)43/h6-7,10-11,18-20,22H,8-9,12-17H2,1-5H3,(H2,36,37,38,39)
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| Chemical Name |
5-bromo-4-N-(5-dimethylphosphorylquinoxalin-6-yl)-2-N-[2-methoxy-5-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine
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| Synonyms |
TQB-3804 TQB3804 TQB 3804
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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 : ~5 mg/mL (~7.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.80 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 12.5 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: ≥ 1.25 mg/mL (1.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 12.5 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: ≥ 1.25 mg/mL (1.80 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 | 1.4397 mL | 7.1984 mL | 14.3968 mL | |
| 5 mM | 0.2879 mL | 1.4397 mL | 2.8794 mL | |
| 10 mM | 0.1440 mL | 0.7198 mL | 1.4397 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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