2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Osimertinib-d6

Osimertinib-d6  (Synonyms: AZD-9291-d6; Mereletinib-d6)

Cat. No.: HY-15772S Purity: 99.97%
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Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

For research use only. We do not sell to patients.

Osimertinib-d<sub>6</sub> Chemical Structure

Osimertinib-d6 Chemical Structure

CAS No. : 1638281-44-3

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5 mg USD 2020 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Osimertinib-d6:

Osimertinib-d6 Related Antibodies

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Description

Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

In Vitro

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16-701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells) [2].
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50 of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50 of 650 and 461 nM in Calu3 and H2073 respectively)[1].
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rate of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Osimertinib-d6 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Dramatically inhibited cell proliferation (IC50=41,26, 41, 31 nM, respectively)

Cell Proliferation Assay[2]

Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferation (IC50 = 6, 7, 74 nM, respectively)

Apoptosis Analysis[2]

Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations)
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferation (IC50 = 16, 701, 230, 38 nM, respectively)

Apoptosis Analysis[2]

Cell Line: Ba/F3 cells(harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Inducted apoptosis with the rate of 40.9% and 90% in EGFR T790M positive mutations cells respectively.
In Vivo

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 day) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration: p.o.; daily for 14 day
Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
Molecular Weight

505.64

Formula

C28H27D6N7O2
CAS No.
Unlabeled CAS

1421373-65-0
Appearance

Solid

Color

White to light yellow

SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C([2H])([2H])[2H])C([2H])([2H])[2H])C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (247.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMSO : 125 mg/mL (247.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9777 mL 9.8885 mL 19.7769 mL
5 mM 0.3955 mL 1.9777 mL 3.9554 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.97%

SDS (252 KB)

COA (258 KB) HNMR (118 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / DMSO 1 mM 1.9777 mL 9.8885 mL 19.7769 mL 49.4423 mL
5 mM 0.3955 mL 1.9777 mL 3.9554 mL 9.8885 mL
10 mM 0.1978 mL 0.9888 mL 1.9777 mL 4.9442 mL
15 mM 0.1318 mL 0.6592 mL 1.3185 mL 3.2962 mL
20 mM 0.0989 mL 0.4944 mL 0.9888 mL 2.4721 mL
25 mM 0.0791 mL 0.3955 mL 0.7911 mL 1.9777 mL
30 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6481 mL
40 mM 0.0494 mL 0.2472 mL 0.4944 mL 1.2361 mL
50 mM 0.0396 mL 0.1978 mL 0.3955 mL 0.9888 mL
60 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL
80 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6180 mL
100 mM 0.0198 mL 0.0989 mL 0.1978 mL 0.4944 mL
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Osimertinib-d6 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Osimertinib-d61638281-44-3AZD-9291-d6Mereletinib-d6EGFREpidermal growth factor receptorErbB-1HER1PC-9H1975Ba/F3 cellscancertumor xenograft modelInhibitorinhibitorinhibit

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