Olafertinib
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MedKoo CAT#: 207019

CAS#: 1660963-42-7

Description: Olafertinib, also known as CK-101 and Olafertinib, is a potent and orally active EGFR mutant-specific inhibitor. CK-101 specifically and covalently binds to and inhibits specific EGFR mutations, with particularly high selectivity against the T790M mutation; this prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, CK-101 may have therapeutic benefits in tumors with T790M-mediated drug resistance.

Chemical Structure

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Olafertinib
CAS# 1660963-42-7
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 207019
Name: Olafertinib
CAS#: 1660963-42-7
Chemical Formula: C29H28F2N6O2
Exact Mass: 530.22
Molecular Weight: 530.580
Elemental Analysis: C, 65.65; H, 5.32; F, 7.16; N, 15.84; O, 6.03

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2850 2 Weeks
1g USD 4250 2 Weeks
2g USD 6450 2 Weeks
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Synonym: CK-101; CK 101; CK101; RX-518; RX 518; RX518; Olafertinib

IUPAC/Chemical Name: N-[3-[2-[2,3-difluoro-4-[4-(2-hydroxyethyl)piperazin-1-yl]anilino]quinazolin-8-yl]phenyl]prop-2-enamide

InChi Key: IDRGFNPZDVBSSE-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H28F2N6O2/c1-2-25(39)33-21-7-3-5-19(17-21)22-8-4-6-20-18-32-29(35-28(20)22)34-23-9-10-24(27(31)26(23)30)37-13-11-36(12-14-37)15-16-38/h2-10,17-18,38H,1,11-16H2,(H,33,39)(H,32,34,35)

SMILES Code: C=CC(NC1=CC=CC(C2=CC=CC3=CN=C(NC4=CC=C(N5CCN(CCO)CC5)C(F)=C4F)N=C23)=C1)=O

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

Shelf Life: >3 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: This agent shows minimal activity against wild-type EGFR (WT EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit WT EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Olafertinib is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively.
In vitro activity: TBD
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 125.0 235.59

Preparing Stock Solutions

The following data is based on the product molecular weight 530.58 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: TBD
In vitro protocol: TBD
In vivo protocol: TBD

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