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

MedKoo CAT#: 577732

CAS#: 1616385-51-3

Description: Bezuclastinib is a c-kit, c-kit D816V, and tyrosine kinase inhibitor.

Chemical Structure

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Bezuclastinib
CAS# 1616385-51-3
Instruction

Theoretical Analysis

MedKoo Cat#: 577732
Name: Bezuclastinib
CAS#: 1616385-51-3
Chemical Formula: C19H17N5O
Exact Mass: 331.14
Molecular Weight: 331.380
Elemental Analysis: C, 68.87; H, 5.17; N, 21.13; O, 4.83

Price and Availability

Size Price Availability Quantity
5mg USD 950 2 Weeks
25mg USD 2250 2 Weeks
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Synonym: Bezuclastinib; CGT9486; CGT 9486; CGT-9486; PLX9486; PLX 9486; PLX-9486

IUPAC/Chemical Name: 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide

InChi Key: NVSHVYGIYPBTEZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H17N5O/c1-11-12(2)23-24-17(11)19(25)21-15-8-14-9-16(22-18(14)20-10-15)13-6-4-3-5-7-13/h3-10H,1-2H3,(H,20,22)(H,21,25)(H,23,24)

SMILES Code: O=C(C1=NNC(C)=C1C)NC2=CN=C(NC(C3=CC=CC=C3)=C4)C4=C2

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: 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:

Preparing Stock Solutions

The following data is based on the product molecular weight 331.38 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. Gebreyohannes YK, Burton EA, Wozniak A, Matusow B, Habets G, Wellens J, Cornillie J, Lin J, Nespi M, Wu G, Zhang C, Bollag G, Debiec-Rychter M, Sciot R, Schöffski P. PLX9486 shows anti-tumor efficacy in patient-derived, tyrosine kinase inhibitor-resistant KIT-mutant xenograft models of gastrointestinal stromal tumors. Clin Exp Med. 2019 May;19(2):201-210. doi: 10.1007/s10238-018-0541-2. Epub 2018 Dec 6. PMID: 30523507.

2. Wagner AJ, Severson PL, Shields AF, Patnaik A, Chugh R, Tinoco G, Wu G, Nespi M, Lin J, Zhang Y, Ewing T, Habets G, Burton EA, Matusow B, Tsai J, Tsang G, Shellooe R, Carias H, Chan K, Rezaei H, Sanftner L, Marimuthu A, Spevak W, Ibrahim PN, Inokuchi K, Alcantar O, Michelson G, Tsiatis AC, Zhang C, Bollag G, Trent JC, Tap WD. Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial. JAMA Oncol. 2021 Sep 1;7(9):1343-1350. doi: 10.1001/jamaoncol.2021.2086. PMID: 34236401; PMCID: PMC8267845.