NVL-520 free base · Synonyms: Zidesamtinib

Zidesamtinib is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions.

For research use only. Not for human or veterinary use.

Target ROS Kinase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

NVL-520 structure

CAS No.: 2739829-00-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 485.00	BP-02045-50mg	In stock	Get quote
100 mg	USD 785.00	BP-02045-100mg	In stock	Get quote
250 mg	USD 1,185.00	BP-02045-250mg	In stock	Get quote
500 mg	USD 1,685.00	BP-02045-500mg	In stock	Get quote
1 g	Inquire	BP-02045-1g	In stock	Inquire

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Description

Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer.

Biological activity

In Vitro Zidesamtinib (72 h) inhibits the growth of seven cell lines expressing wild-type ROS1 fusions, with average IC50s of 0.4 nM. Zidesamtinib (72 h) inhibits the growth of six cell lines harboring ROS1 fusions with the G2032R mutation, with average IC50s of 1.6 nM. Zidesamtinib (72 h) potently inhibits the non-G2032R ROS1 mutants, with IC50s ≤ 1.5 nM. Zidesamtinib (10-1000 nM; 4 weeks) suppresses colony formation in NIH3T3 cells expressing wild-type ROS1 fusions and expressing ROS1 fusions with G2032R. In Vivo Zidesamtinib (0.04-15 mg/kg; p.o. twice daily for 28 d) induces tumor regression at all doses ≥0.2 mg/kg in wild-type ROS1 xenograft models.

Identifiers

SMILES: CCN1C2=C(CC3=NN(N=C3C4=C(C=C(C=C4)F)[C@H](OC5=C(N=CC2=C5)N)C)C)C=N1
InChIKey: DTWUUAFTYSMNQX-GFCCVEGCSA-N

Specifications

MW (average): 419.4548
Formula: C₂₂H₂₂FN₇O
CAS No.: 2739829-00-4
Physical state: Solid
Color: Off-white to light yellow
Shipping: 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: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 50 mg/mL

Documents

References

[1]. Drilon A, et, al. NVL-520 is a selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations. Cancer Discov. 2022 Dec 13;CD-22-0968.

Same target

Search ROS Kinase

Same research area

Search Cancer