Transtinib

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

Hodoodo CAT#: H407260

CAS#: 1246089-27-9

Description: Transtinib is a potent and irreversible EGFR tyrosine kinase inhibitors (EGFR-TKIs) with activity against L858R/T790M mutant NSCLC cell lines and xenografts. Transtinib displayed strong anti-proliferative activity against the H1975 and A431 cell lines with IC50 values of 34 nM and 62 nM, respectively. In xenograft models, Transtinib significantly decreases tumor size for a prolonged period of time. Transtinib is a potential cancer therapeutic drug lead for the inhibition of mutant EGFR to overcome the development of resistance.

Chemical Structure

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Transtinib
CAS# 1246089-27-9
Instruction

Theoretical Analysis

Hodoodo Cat#: H407260
Name: Transtinib
CAS#: 1246089-27-9
Chemical Formula: C30H29ClFN5O3
Exact Mass: 561.19
Molecular Weight: 562.042
Elemental Analysis: C, 64.11; H, 5.20; Cl, 6.31; F, 3.38; N, 12.46; O, 8.54

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Transtinib

IUPAC/Chemical Name: (S,E)-N-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-7-ethoxyquinazolin-6-yl)-3-(pyrrolidin-2-yl)acrylamide

InChi Key: XDPSIOSBWCREAL-ZUURVNMSSA-N

InChi Code: InChI=1S/C30H29ClFN5O3/c1-2-39-28-16-25-23(15-26(28)37-29(38)11-9-21-7-4-12-33-21)30(35-18-34-25)36-22-8-10-27(24(31)14-22)40-17-19-5-3-6-20(32)13-19/h3,5-6,8-11,13-16,18,21,33H,2,4,7,12,17H2,1H3,(H,37,38)(H,34,35,36)/b11-9+/t21-/m0/s1

SMILES Code: O=C(NC1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1OCC)/C=C/[C@H]5NCCC5

Appearance: Solid powder

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: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 562.04 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:
In vitro protocol:
In vivo protocol:

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1: Hu P, Han D, Ruan R, Zheng LM, Tzeng CM. Transtinib, a potent tyrosine kinase
inhibitor inhibits L858R/T790M mutant NSCLC cell lines and xenografts.
Oncotarget. 2016 Feb 2. doi: 10.18632/oncotarget.7140. [Epub ahead of print]
PubMed PMID: 26848869.