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MedKoo Cat#: 127052 | Name: AZ14133346

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZ14133346 is a potent and selective inhibitor of EGFR Exon20 insertions (IC50 = 85 nM). AZ14133346 has demonstrated encouraging efficacy in NSCLC EGFR CRISPR-engineered H2073 xenografts that carry an SVD Exon20 insertion and reduced efficacy in a H2073 wild-type EGFR xenograft model compared to CLN-081, indicating that AZ14133346 may have lower EGFR wild-type associated toxicity.

Chemical Structure

AZ14133346
AZ14133346
CAS#N/A

Theoretical Analysis

MedKoo Cat#: 127052

Name: AZ14133346

CAS#: N/A

Chemical Formula: C29H27N5O2

Exact Mass: 477.2165

Molecular Weight: 477.57

Elemental Analysis: C, 72.94; H, 5.70; N, 14.66; O, 6.70

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
AZ14133346; AZ-14133346; AZ 14133346
IUPAC/Chemical Name
(S,E)-1-(3-(3-(3-(2-(5-cyclopropyloxazol-2-yl)vinyl)phenyl)-4-(pyridin-4-yl)-1H-pyrazol-1-yl)pyrrolidin-1-yl)prop-2-en-1-one
InChi Key
SVLLKLFGGWAXTK-OKHPUOTASA-N
InChi Code
InChI=1S/C29H27N5O2/c1-2-28(35)33-15-12-24(18-33)34-19-25(21-10-13-30-14-11-21)29(32-34)23-5-3-4-20(16-23)6-9-27-31-17-26(36-27)22-7-8-22/h2-6,9-11,13-14,16-17,19,22,24H,1,7-8,12,15,18H2/b9-6+/t24-/m0/s1
SMILES Code
O=C(C=C)N(CC1)C[C@H]1N(N=C2C3=CC=CC(/C=C/C4=NC=C(C5CC5)O4)=C3)C=C2C6=CC=NC=C6
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 477.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations Clare Thomson, Peter Barton, Erin Braybrooke, Nicola Colclough, Zhiqiang Dong, Laura Evans, Nicolas Floc’h, Carine Guérot, David Hargreaves, Puneet Khurana, Songlei Li, Xiuwei Li, Andrew Lister, William McCoull, Lisa McWilliams, Jonathan P. Orme, Martin J. Packer, Aisha M. Swaih, Richard A. Ward, Poppy Winlow, and Yang Ye Journal of Medicinal Chemistry Article ASAP DOI: 10.1021/acs.jmedchem.4c00227