BDTX-1535
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 207191

CAS#: 2607829-38-7

Description: BDTX-1535 is a potent, selective, brain penetrant and irreversible MasterKey inhibitor of EGFR mutations that expressed in glioblastoma multiforme (GBM) and intrinsic and acquired resistance EGFR mutations in non-small cell lung cancer (NSCLC). BDTX-1535 selectively targets, irreversibly binds to, and inhibits the activity of various EGFR alterations and mutations, including certain intrinsic and acquired resistance mutations. This prevents EGFR-mediated signaling in susceptible tumor cells. BDTX-1535 may mitigate resistance to osimertinib, the standard of care for EGFR-mutant non-small cell lung cancer. It could also potentially treat central nervous system metastases, having shown preclinical efficacy in glioblastoma.

Chemical Structure

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BDTX-1535
CAS# 2607829-38-7
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 207191
Name: BDTX-1535
CAS#: 2607829-38-7
Chemical Formula: C30H30ClFN6O2
Exact Mass: 560.21
Molecular Weight: 561.058
Elemental Analysis: C, 64.22; H, 5.39; Cl, 6.32; F, 3.39; N, 14.98; O, 5.70

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to ship
10mg USD 250 Ready to Ship
25mg USD 450 Ready to Ship
50mg USD 750 Ready to Ship
100mg USD 1350 Ready to Ship
200mg USD 2150 Ready to Ship
500mg USD 4250 Ready to Ship
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Synonym: BDTX-1535; BDTX 1535; BDTX1535;

IUPAC/Chemical Name: (2E)-N-[4-[(3-Chloro-2-fluorophenyl)amino]-7-[2-[(1R,5S)-3-methyl-3-azabicyclo[3.1.0]hex-1-yl]ethynyl]-6-quinazolinyl]-4-(4-morpholinyl)-2-butenamide

InChi Key: LMOVDLRMIRLIJF-TUVXKDNKSA-N

InChi Code: InChI=1S/C30H30ClFN6O2/c1-37-17-21-16-30(21,18-37)8-7-20-14-26-22(29(34-19-33-26)36-24-5-2-4-23(31)28(24)32)15-25(20)35-27(39)6-3-9-38-10-12-40-13-11-38/h2-6,14-15,19,21H,9-13,16-18H2,1H3,(H,35,39)(H,33,34,36)/b6-3+/t21-,30+/m1/s1

SMILES Code: O=C(NC1=CC2=C(NC3=CC=CC(Cl)=C3F)N=CN=C2C=C1C#C[C@]45CN(C)C[C@@]4([H])C5)/C=C/CN6CCOCC6

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:

Product Data:
Product Data
Certificate of Analysis:
View CoA: current batch, Lot#C23G05C10
QC Data:
test
Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)
Instruction:
View handling instruction
Biological target: PY-60 is a specific activator of YAP transcriptional activity that targets annexin ANXA2 (Kd = 1.4 µM). PY-60 directly binds to ANXA2 and antagonizes its repression of YAP activity.
In vitro activity: To be determined
In vivo activity: BDTX-1535 may mitigate resistance to osimertinib, the standard of care for EGFR-mutant non-small cell lung cancer. It could also potentially treat central nervous system metastases, since it demonstrated preclinical efficacy in glioblastoma. Reference: Cancer Discov. 2021 Dec 1;11(12):2952-2953. https://pubmed.ncbi.nlm.nih.gov/34702733/

Preparing Stock Solutions

The following data is based on the product molecular weight 561.06 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
Formulation protocol: 1. BDTX-1535 Goes after Osimertinib Resistance. Cancer Discov. 2021 Dec 1;11(12):2952-2953. doi: 10.1158/2159-8290.CD-NB2021-0395. PMID: 34702733.
In vitro protocol: To be determined
In vivo protocol: 1. BDTX-1535 Goes after Osimertinib Resistance. Cancer Discov. 2021 Dec 1;11(12):2952-2953. doi: 10.1158/2159-8290.CD-NB2021-0395. PMID: 34702733.

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1. BDTX-1535 Goes after Osimertinib Resistance. Cancer Discov. 2021 Dec 1;11(12):2952-2953. doi: 10.1158/2159-8290.CD-NB2021-0395. PMID: 34702733.