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MedKoo Cat#: 407139 | Name: BBT-594
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Description:

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

BBT594, also known as NVP-BBT594, is potent and selective RET and JAK2 inhibitor. NVP-BBT594 impairs GDNF-RET signaling and GDNF-dependent growth of MCF7-LTED cells. NVP-BBT594 targets GDNF-RET signaling and sensitizes MCF7-2A cells to letrozole treatment. GDNF-RET signaling as a rational therapeutic target may be useful to combat or delay the onset of AI resistance in breast cancer.

Chemical Structure

BBT-594
BBT-594
CAS# 882405-89-2

Theoretical Analysis

MedKoo Cat#: 407139

Name: BBT-594

CAS#: 882405-89-2

Chemical Formula: C28H30F3N7O3

Exact Mass: 569.2362

Molecular Weight: 569.59

Elemental Analysis: C, 59.04; H, 5.31; F, 10.01; N, 17.21; O, 8.43

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,950.00 Ready to ship
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Synonym
BBT-594; BBT-594; BBT-594; NVP-BBT594; NVP BBT594; NVP BBT-594.
IUPAC/Chemical Name
5-((6-acetamidopyrimidin-4-yl)oxy)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)indoline-1-carboxamide
InChi Key
VQLNKQZLPGLOSI-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H30F3N7O3/c1-18(39)34-25-15-26(33-17-32-25)41-22-5-6-24-19(13-22)7-8-38(24)27(40)35-21-4-3-20(23(14-21)28(29,30)31)16-37-11-9-36(2)10-12-37/h3-6,13-15,17H,7-12,16H2,1-2H3,(H,35,40)(H,32,33,34,39)
SMILES Code
O=C(N1CCC2=C1C=CC(OC3=NC=NC(NC(C)=O)=C3)=C2)NC4=CC=C(CN5CCN(C)CC5)C(C(F)(F)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, 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
More Info
Biological target:
BBT594 is a potent receptor tyrosine kinase RET inhibitor.
In vitro activity:
In contrast, the same concentration range of type II JAK2 inhibitor BBT594 potently inhibited growth of JAK2-driven cell lines with an IC50 of 0.1 ± 0.005 μM in MHH-CALL-4 and 0.1± 0.008 μM in MUTZ-5 (Figure 1A-1B). In non–JAK2-driven REH cells, only high concentrations exceeding 1μM of BB T594 showed minimal growth-inhibitory effects, possible due to off-target activity (Supplementary Figure 1C). Reference: Oncotarget. 2018 Jan 30; 9(8): 8027–8041. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5814279/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 33.0 57.94
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 569.59 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:
1. Zhang Q, Shi C, Han L, Jain N, Roberts KG, Ma H, Cai T, Cavazos A, Tabe Y, Jacamo RO, Mu H, Zhao Y, Wang J, Wu SC, Cao F, Zeng Z, Zhou J, Mi Y, Jabbour EJ, Levine R, Tasian SK, Mullighan CG, Weinstock DM, Fruman DA, Konopleva M. Inhibition of mTORC1/C2 signaling improves anti-leukemia efficacy of JAK/STAT blockade in CRLF2 rearranged and/or JAK driven Philadelphia chromosome-like acute B-cell lymphoblastic leukemia. Oncotarget. 2018 Jan 17;9(8):8027-8041. doi: 10.18632/oncotarget.24261. PMID: 29487712; PMCID: PMC5814279. 2. Morandi A, Martin LA, Gao Q, Pancholi S, Mackay A, Robertson D, Zvelebil M, Dowsett M, Plaza-Menacho I, Isacke CM. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95. doi: 10.1158/0008-5472.CAN-12-4265. Epub 2013 May 6. PMID: 23650283; PMCID: PMC3686594.
In vitro protocol:
1. Zhang Q, Shi C, Han L, Jain N, Roberts KG, Ma H, Cai T, Cavazos A, Tabe Y, Jacamo RO, Mu H, Zhao Y, Wang J, Wu SC, Cao F, Zeng Z, Zhou J, Mi Y, Jabbour EJ, Levine R, Tasian SK, Mullighan CG, Weinstock DM, Fruman DA, Konopleva M. Inhibition of mTORC1/C2 signaling improves anti-leukemia efficacy of JAK/STAT blockade in CRLF2 rearranged and/or JAK driven Philadelphia chromosome-like acute B-cell lymphoblastic leukemia. Oncotarget. 2018 Jan 17;9(8):8027-8041. doi: 10.18632/oncotarget.24261. PMID: 29487712; PMCID: PMC5814279. 2. Morandi A, Martin LA, Gao Q, Pancholi S, Mackay A, Robertson D, Zvelebil M, Dowsett M, Plaza-Menacho I, Isacke CM. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95. doi: 10.1158/0008-5472.CAN-12-4265. Epub 2013 May 6. PMID: 23650283; PMCID: PMC3686594.
In vivo protocol:
TBD
1: Zhang Q, Shi C, Han L, Jain N, Roberts KG, Ma H, Cai T, Cavazos A, Tabe Y, Jacamo RO, Mu H, Zhao Y, Wang J, Wu SC, Cao F, Zeng Z, Zhou J, Mi Y, Jabbour EJ, Levine R, Tasian SK, Mullighan CG, Weinstock DM, Fruman DA, Konopleva M. Inhibition of mTORC1/C2 signaling improves anti-leukemia efficacy of JAK/STAT blockade in CRLF2 rearranged and/or JAK driven Philadelphia chromosome-like acute B-cell lymphoblastic leukemia. Oncotarget. 2018 Jan 17;9(8):8027-8041. doi: 10.18632/oncotarget.24261. eCollection 2018 Jan 30. PubMed PMID: 29487712; PubMed Central PMCID: PMC5814279. 2: Kong X, Sun H, Pan P, Li D, Zhu F, Chang S, Xu L, Li Y, Hou T. How Does the L884P Mutation Confer Resistance to Type-II Inhibitors of JAK2 Kinase: A Comprehensive Molecular Modeling Study. Sci Rep. 2017 Aug 22;7(1):9088. doi: 10.1038/s41598-017-09586-3. PubMed PMID: 28831147; PubMed Central PMCID: PMC5567357. 3: Andreucci E, Francica P, Fearns A, Martin LA, Chiarugi P, Isacke CM, Morandi A. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancer xenografts. Oncotarget. 2016 Dec 6;7(49):80543-80553. doi: 10.18632/oncotarget.11826. PubMed PMID: 27602955; PubMed Central PMCID: PMC5348339. 4: Morandi A, Martin LA, Gao Q, Pancholi S, Mackay A, Robertson D, Zvelebil M, Dowsett M, Plaza-Menacho I, Isacke CM. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95. doi: 10.1158/0008-5472.CAN-12-4265. Epub 2013 May 6. PubMed PMID: 23650283; PubMed Central PMCID: PMC3686594.