WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130070
CAS#: 2739829-00-4
Description: Zidesamtinib, also known as NVL-520, is a tyrosine kinase inhibitor, specifically ROS1, with potential as an antineoplastic agent. NVL-520 is a rationally designed macrocycle with >50-fold ROS1 selectivity over 98% of the kinome tested. It is active in vitro against diverse ROS1 fusions and resistance mutations and exhibits 10- to 1,000-fold improved potency for the ROS1 G2032R solvent-front mutation over crizotinib, entrectinib, lorlatinib, taletrectinib, and repotrectinib. In vivo, it induces tumor regression in G2032R-inclusive intracranial and patient-derived xenograft models. Importantly, NVL-520 has an ∼100-fold increased potency for ROS1 and ROS1 G2032R over TRK.
Hodoodo Cat#: H130070
Name: Zidesamtinib
CAS#: 2739829-00-4
Chemical Formula: C22H22FN7O
Exact Mass: 419.19
Molecular Weight: 419.460
Elemental Analysis: C, 63.00; H, 5.29; F, 4.53; N, 23.37; O, 3.81
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Synonym: Zidesamtinib; NVL-520; NVL520; NVL 520;
IUPAC/Chemical Name: (6R)-22-ethyl-54-fluoro-42,6-dimethyl-22H,42 H-7-oxa1(3,5)-pyridina-2(3,4)-pyrazola-4(4,5)-[1,2,3]triazola5(1,2)-benzenacycloheptaphan-16-amine
InChi Key: DTWUUAFTYSMNQX-GFCCVEGCSA-N
InChi Code: InChI=1S/C22H22FN7O/c1-4-30-21-13(11-26-30)7-18-20(28-29(3)27-18)16-6-5-15(23)9-17(16)12(2)31-19-8-14(21)10-25-22(19)24/h5-6,8-12H,4,7H2,1-3H3,(H2,24,25)/t12-/m1/s1
SMILES Code: FC1=CC([C@](OC2=C(N=CC3=C2)N)(C)[H])=C(C=C1)C4=NN(N=C4CC5=C3N(N=C5)CC)C
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 419.46 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.
| 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: |
1. Drilon A, Horan JC, Tangpeerachaikul A, Besse B, Ou SI, Gadgeel SM, Camidge DR, van der Wekken AJ, Nguyen-Phuong L, Acker A, Keddy C, Nicholson KS, Yoda S, Mente S, Sun Y, Soglia JR, Kohl NE, Porter JR, Shair MD, Zhu V, Davare MA, Hata AN, Pelish HE, Lin JJ. NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations. Cancer Discov. 2023 Mar 1;13(3):598-615. doi: 10.1158/2159-8290.CD-22-0968. PMID: 36511802; PMCID: PMC9975673.
2. Ou SI, Hagopian GG, Zhang SS, Nagasaka M. Comprehensive review of ROS1 tyrosine kinase inhibitors (TKIs)-classified by structural designs and mutation spectrum [solvent front mutation (G2032R) and central β-sheet 6 (Cβ6) mutation (L2086F)]. J Thorac Oncol. 2023 Dec 7:S1556-0864(23)02413-9. doi: 10.1016/j.jtho.2023.12.008. Epub ahead of print. PMID: 38070596.
