MedKoo Cat#: 462508 | Name: Taletrectinib free base
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Description:

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

Taletrectinib, also known as DS-6051B, is an orally available inhibitor of the receptor tyrosine kinases C-ros oncogene 1 (ROS1) and the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, with potential antineoplastic activity. Upon oral administration, DS-6051b binds to and inhibits ROS1 and the NTRK family members. This inhibition leads to a disruption of ROS1- and NTRK-mediated signaling and eventually inhibits the growth of tumor cells that are overexpressing ROS1 and/or NTRKs. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells. NTRK mutations or rearrangements play a key role in cancer progression.

Chemical Structure

Taletrectinib free base
Taletrectinib free base
CAS#1505514-27-1 (free base)

Theoretical Analysis

MedKoo Cat#: 462508

Name: Taletrectinib free base

CAS#: 1505514-27-1 (free base)

Chemical Formula: C23H24FN5O

Exact Mass: 405.1965

Molecular Weight: 405.48

Elemental Analysis: C, 68.13; H, 5.97; F, 4.69; N, 17.27; O, 3.95

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
10mg USD 750.00 2 Weeks
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Synonym
Taletrectinib; DS-6051b; DS6051b; DS 6051b; AB-106; AB106; AB 106;
IUPAC/Chemical Name
3-{4-[(2R)-2-aminopropoxy]phenyl}-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine
InChi Key
HEVHTYMYEMEBPX-HZPDHXFCSA-N
InChi Code
InChI=1S/C23H24FN5O/c1-15(25)14-30-20-8-6-17(7-9-20)21-13-26-23-11-10-22(28-29(21)23)27-16(2)18-4-3-5-19(24)12-18/h3-13,15-16H,14,25H2,1-2H3,(H,27,28)/t15-,16-/m1/s1
SMILES Code
C[C@@H](NC1=NN2C(C=C1)=NC=C2C3=CC=C(OC[C@H](N)C)C=C3)C4=CC=CC(F)=C4
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

Preparing Stock Solutions

The following data is based on the product molecular weight 405.48 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
1: Ruzzi F, Angelicola S, Landuzzi L, Nironi E, Semprini MS, Scalambra L, Altimari A, Gruppioni E, Fiorentino M, Giunchi F, Ferracin M, Astolfi A, Indio V, Ardizzoni A, Gelsomino F, Nanni P, Lollini PL, Palladini A. ADK-VR2, a cell line derived from a treatment-naïve patient with SDC4-ROS1 fusion- positive primarily crizotinib-resistant NSCLC: a novel preclinical model for new drug development of ROS1-rearranged NSCLC. Transl Lung Cancer Res. 2022 Nov;11(11):2216-2229. doi: 10.21037/tlcr-22-163. PMID: 36519016; PMCID: PMC9742620. 2: Ou SI, Fujiwara Y, Shaw AT, Yamamoto N, Nakagawa K, Fan F, Hao Y, Gao Y, Jänne PA, Seto T. Efficacy of Taletrectinib (AB-106/DS-6051b) in ROS1+ NSCLC: An Updated Pooled Analysis of U.S. and Japan Phase 1 Studies. JTO Clin Res Rep. 2020 Oct 21;2(1):100108. doi: 10.1016/j.jtocrr.2020.100108. PMID: 34589973; PMCID: PMC8474193. 3: Sehgal K, Piper-Vallillo AJ, Viray H, Khan AM, Rangachari D, Costa DB. Cases of ROS1-rearranged lung cancer: when to use crizotinib, entrectinib, lorlatinib, and beyond? Precis Cancer Med. 2020 Jun;3:17. doi: 10.21037/pcm-2020-potb-02. Epub 2020 Jun 15. PMID: 32776005; PMCID: PMC7410006. 4: Patil T, Simons E, Mushtaq R, Pacheco JM, Doebele RC, Bowles DW. Targeted therapies for ROS1-rearranged non-small cell lung cancer. Drugs Today (Barc). 2019 Oct;55(10):641-652. doi: 10.1358/dot.2019.55.10.3030646. PMID: 31720561. 5: Katayama R, Gong B, Togashi N, Miyamoto M, Kiga M, Iwasaki S, Kamai Y, Tominaga Y, Takeda Y, Kagoshima Y, Shimizu Y, Seto Y, Oh-Hara T, Koike S, Nakao N, Hanzawa H, Watanabe K, Yoda S, Yanagitani N, Hata AN, Shaw AT, Nishio M, Fujita N, Isoyama T. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019 Aug 9;10(1):3604. doi: 10.1038/s41467-019-11496-z. PMID: 31399568; PMCID: PMC6688997. 6: Fujiwara Y, Takeda M, Yamamoto N, Nakagawa K, Nosaki K, Toyozawa R, Abe C, Shiga R, Nakamaru K, Seto T. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018 May 4;9(34):23729-23737. doi: 10.18632/oncotarget.25263. PMID: 29805770; PMCID: PMC5955103. 7: Khotskaya YB, Holla VR, Farago AF, Mills Shaw KR, Meric-Bernstam F, Hong DS. Targeting TRK family proteins in cancer. Pharmacol Ther. 2017 May;173:58-66. doi: 10.1016/j.pharmthera.2017.02.006. Epub 2017 Feb 4. PMID: 28174090.