Dubermatinib
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MedKoo CAT#: 206462

CAS#: 1341200-45-0

Description: Dubermatinib, also known as TP-0903, is a potent and selective AXL inhibitor. TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges. Combination of TP-0903 with BTK inhibitors augments CLL B-cell apoptosis AXL overexpression is a reoccurring theme observed in multiple tumor types that have acquired resistance to various agents. Treatment of cancer cells with TP-0903 reverses the mesenchymal phenotype in multiple models and sensitizes cancer cells to treatment with other targeted agents. Administration of TP-0903 either as a single agent or in combination with BTK inhibitors may be effective in treating patients with CLL.


Chemical Structure

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Dubermatinib
CAS# 1341200-45-0

Theoretical Analysis

MedKoo Cat#: 206462
Name: Dubermatinib
CAS#: 1341200-45-0
Chemical Formula: C24H30ClN7O2S
Exact Mass: 515.18702
Molecular Weight: 516.06
Elemental Analysis: C, 55.86; H, 5.86; Cl, 6.87; N, 19.00; O, 6.20; S, 6.21

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1550 Same day
1g USD 2450 Same day
2g USD 3650 Same day
5g USD 6850 2 weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-09. Prices are subject to change without notice.

Dubermatinib, purity > 97%, is in stock. The same day shipping out after order is received.

Synonym: TP-0903; TP 0903; TP0903; Dubermatinib

IUPAC/Chemical Name: 2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide

InChi Key: YUAALFPUEOYPNX-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)

SMILES Code: O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(CN4CCN(C)CC4)C=C3)=NC=C2Cl)(N(C)C)=O

Appearance:
Off white to orange solid powder

Purity:
>97% (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, not in water

Shelf Life:
>2 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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO, not in water 100.0

Preparing Stock Solutions

The following data is based on the product molecular weight 516.06 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Park IK, Mundy-Bosse B, Whitman SP, Zhang X, Warner SL, Bearss DJ, Blum W, Marcucci G, Caligiuri MA. Receptor tyrosine kinase Axl is required for resistance of leukemic cells to FLT3-targeted therapy in acute myeloid leukemia. Leukemia. 2015 Jun 19. doi: 10.1038/leu.2015.147. [Epub ahead of print] PubMed PMID: 26172401.

2: Sinha S, Boysen J, Nelson M, Secreto C, Warner SL, Bearss DJ, Lesnick C, Shanafelt TD, Kay NE, Ghosh AK. Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors. Clin Cancer Res. 2015 May 1;21(9):2115-26. doi: 10.1158/1078-0432.CCR-14-1892. Epub 2015 Feb 11. PubMed PMID: 25673699; PubMed Central PMCID: PMC4479154.